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IdentificationPharmacologyInteractionsReferencesTrialsEconomicsPropertiesSpectraTaxonomyFormestane
Identification
- Name
- Formestane
- Accession Number
- DB08905
- Type
- Small Molecule
- Groups
- Approved, Investigational, Withdrawn
- Description
Formestane was the first selective, type I, steroidal aromatase inhibitor used in the treatment of estrogen-receptor positive breast cancer in post-menopausal women. Formestane suppresses estrogen production from anabolic steroids or prohormones. It also acts as a prohormone to 4-hydroxytestosterone, an active steroid which displays weak androgenic activity in addition to acting as a mild aromatase inhibitor. It is listed as a prohibited substance by the World Anti-Doping Agency for use in athletes.
Formestane has poor oral bioavailability, and thus must be administered forthnightly (bi-weekly) by intramuscular injection. Some clinical data has suggested that the clinically recommended dose of 250mg was too low. With the discovery of newer, non-steroidal and steroidal, aromatase inhibitors which were orally active and less expensive than formestane, formestane lost popularity.
Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance to the regulations of the World Anti-Doping Agency. It is not US FDA approved, and the intramuscular injection form of formestane (Lentaron) which was approved in Europe has been withdrawn.
- Structure
Structure for DB08905 (Formestane)
- Synonyms
- 4-hydroxy-4-androstene-3,17-dione
- 4-Hydroxy-delta(4)-androstenedione
- 4-hydroxy-Δ4-androstenedione
- 4-hydroxyandrostenedione
- 4-OH-A
- 4-OHAD
- Formestano
- Formestanum
- External IDs
- CGP 32349 / CGP-32349
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Lentaron Formestane (250 mg) + Sodium Chloride (.9 %) Liquid; Powder, for solution Intramuscular Novartis 1994-12-31 1999-08-04 Canada 
- International/Other Brands
- Lentaron
- Categories
- 17-Ketosteroids
- Adrenal Cortex Hormones
- Androstanes
- Androstenes
- Antineoplastic Agents
- Antineoplastic and Immunomodulating Agents
- Aromatase Inhibitors
- Endocrine Therapy
- Enzyme Inhibitors
- Estrogen Antagonists
- Gonadal Hormones
- Gonadal Steroid Hormones
- Hormone Antagonists
- Hormone Antagonists and Related Agents
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Ketosteroids
- Steroid Synthesis Inhibitors
- Steroids
- Testosterone Congeners
- UNII
- PUB9T8T355
- CAS number
- 566-48-3
- Weight
- Average: 302.4079
Monoisotopic: 302.188194698 - Chemical Formula
- C19H26O3
- InChI Key
- OSVMTWJCGUFAOD-KZQROQTASA-N
- InChI
- InChI=1S/C19H26O3/c1-18-10-8-15(20)17(22)14(18)4-3-11-12-5-6-16(21)19(12,2)9-7-13(11)18/h11-13,22H,3-10H2,1-2H3/t11-,12-,13-,18+,19-/m0/s1
- IUPAC Name
- (1S,2R,10R,11S,15S)-6-hydroxy-2,15-dimethyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadec-6-ene-5,14-dione
- SMILES
- [H][[email protected]@]12CCC(=O)[[email protected]@]1(C)CC[[email protected]@]1([H])[[email protected]@]2([H])CCC2=C(O)C(=O)CC[[email protected]]12C
Pharmacology
- Indication
For the treatment of estrogen-receptor positive breast cancer in post-menopausal women.
- Structured Indications
- Not Available
- Pharmacodynamics
By significantly reducing estrogen levels in the bloodstream, formestane may exhibit antitumor activity.
In one trial involving 147 postmenopausal females with advanced breast cancers resistant to standard therapies, 22% of patients achieved a partial response, while another 20% achieved disease stabilization. [3]
In comparative trials comparing a non-steroidal aromatase inhibitor, anastrozole, with formestane, it was found that anastrozole was more effective and consistent at suppressing estrogen levels in the body. However, these results were of unverified clinical significance. [5]
- Mechanism of action
Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production.
Breast cancer may be estrogen sensitive or insensitive. A majority of breast cancers are estrogen sensitive. Estrogen sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone sensitive breast cancers.
Formestane has been targeted specifically for the treatment of postmenopausal women. Unlike premenopausal women who produce most estrogen in the ovaries, postmenopausal women produce most estrogen in peripheral tissues with the help of the aromatase enzyme. Formestane, an aromatase inhibitor, can thus help to decrease the local production of estrogen by blocking the aromatase enzyme in peripheral tissues (ie. adispose tissue of the breast) to treat hormone sensitive breast cancer.
- Absorption
Formestane has poor oral bioavailability, but is fully bioavailable when administered via the established intramuscular route. The AUC after an intravenous pulse dose does not vary considerably from that of an intramuscular dose.
Within 24-48 h of the first dose of intramuscular formestane, a C(max) of 48.0 +/- 20.9 nmol/l was achieved in one study. [2]
- Volume of distribution
Vd = 1.8 L/kg; widely distributed to organs and tissues when delivered intravenously. [2]
- Protein binding
- Not Available
- Metabolism
Hepatic metabolism. Phase I of metabolism is mainly reductive in nature. The reduction products 3 beta-hydroxy-5alpha-androstane-4,17-dione and 3alpha-hydroxy-5beta-androstane-4,17-dione are produced, and further reduced. A notable step in the process of metabolism is a keto reduction on carbon number three of the molecule. The main metabolite which is produced from formestane is 4-hydroyxyandrost-4-ene-3,17-dione-4-glucuronide.
The oxidation products identified were 4-hydroxyandrosta-4,6-diene-3,17-dione and 4-hydroxyandrosta-1,4-diene-3,17-dione.
In phase II, conjugation was diverse and included sulfatation and glucuronidation. 4-hydroxytestosterone, the 17-hydroxylated analog to formestane, was identified as one particular metabolite found in women's urine. This finding was the result of an oral administration of 500mg of formestane in women.
- Route of elimination
Renal elimination. >95% in urine, <5% in feces.
- Half life
Terminal plasma elimination half life of 18 minutes, when delivered intravenously. [2]
- Clearance
Plasma clearance is approximately 4.2 L/(h kg), when delivered intravenously.
In women, following a 500mg dose of formestane, 20% was excreted as glucuronide within the first 24 hours. [1]
One long term metabolite (3beta,4alpha-dihydroxy-5alpha-androstan-17-one) can be detected for 90 hours. A longer detection time is possible with more sensitive technology, which may be of utility in sports drug testing. [1]
- Toxicity
- Not Available
- Affected organisms
- Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
Drug Interaction Drug group (4R)-limonene The risk or severity of adverse effects can be increased when (4R)-limonene is combined with Formestane. Investigational 1,10-Phenanthroline The risk or severity of adverse effects can be increased when Formestane is combined with 1,10-Phenanthroline. Experimental Aceclofenac The risk or severity of adverse effects can be increased when Aceclofenac is combined with Formestane. Approved, Investigational Acemetacin The risk or severity of adverse effects can be increased when Acemetacin is combined with Formestane. Approved, Experimental, Investigational Acetyldigitoxin Acetyldigitoxin may decrease the cardiotoxic activities of Formestane. Approved Acetyldigoxin Acetyldigoxin may decrease the cardiotoxic activities of Formestane. Experimental Acetylsalicylic acid The risk or severity of adverse effects can be increased when Acetylsalicylic acid is combined with Formestane. Approved, Vet Approved Adapalene The risk or severity of adverse effects can be increased when Adapalene is combined with Formestane. Approved Alclofenac The risk or severity of adverse effects can be increased when Alclofenac is combined with Formestane. Approved, Withdrawn Aldesleukin Formestane may decrease the antineoplastic activities of Aldesleukin. Approved Almasilate The bioavailability of Formestane can be decreased when combined with Almasilate. Approved, Experimental Alminoprofen The risk or severity of adverse effects can be increased when Alminoprofen is combined with Formestane. Experimental Aloglutamol The bioavailability of Formestane can be decreased when combined with Aloglutamol. Approved Aloxiprin The risk or severity of adverse effects can be increased when Aloxiprin is combined with Formestane. Experimental Aluminium The bioavailability of Formestane can be decreased when combined with Aluminium. Approved, Investigational Aluminium acetoacetate The bioavailability of Formestane can be decreased when combined with Aluminium acetoacetate. Experimental Aluminium glycinate The bioavailability of Formestane can be decreased when combined with Aluminium glycinate. Experimental Aluminum hydroxide The bioavailability of Formestane can be decreased when combined with Aluminum hydroxide. Approved, Investigational Ambenonium The risk or severity of adverse effects can be increased when Formestane is combined with Ambenonium. Approved Aminosalicylic Acid The risk or severity of adverse effects can be increased when Aminosalicylic Acid is combined with Formestane. Approved Amiodarone The serum concentration of Formestane can be increased when it is combined with Amiodarone. Approved, Investigational Amphotericin B Formestane may increase the hypokalemic activities of Amphotericin B. Approved, Investigational Ancestim The risk or severity of cytotoxicity can be increased when Ancestim is combined with Formestane. Approved, Investigational, Withdrawn Andrographolide The risk or severity of adverse effects can be increased when Andrographolide is combined with Formestane. Investigational Anisodamine The risk or severity of adverse effects can be increased when Anisodamine is combined with Formestane. Investigational Anthrax immune globulin human The risk or severity of adverse effects can be increased when Formestane is combined with Anthrax immune globulin human. Approved Antipyrine The risk or severity of adverse effects can be increased when Antipyrine is combined with Formestane. Approved, Investigational Apalutamide The serum concentration of Formestane can be decreased when it is combined with Apalutamide. Approved, Investigational Apocynin The risk or severity of adverse effects can be increased when Apocynin is combined with Formestane. Investigational Apremilast The risk or severity of adverse effects can be increased when Apremilast is combined with Formestane. Approved, Investigational Aprepitant The serum concentration of Formestane can be increased when it is combined with Aprepitant. Approved, Investigational Atazanavir The serum concentration of Formestane can be increased when it is combined with Atazanavir. Approved, Investigational Atracurium besylate Atracurium besylate may increase the adverse neuromuscular activities of Formestane. Approved Azapropazone The risk or severity of adverse effects can be increased when Azapropazone is combined with Formestane. Withdrawn Azelastine The risk or severity of adverse effects can be increased when Azelastine is combined with Formestane. Approved Azosemide Formestane may increase the hypokalemic activities of Azosemide. Investigational Bacillus calmette-guerin substrain connaught live antigen The risk or severity of adverse effects can be increased when Formestane is combined with Bacillus calmette-guerin substrain connaught live antigen. Approved, Investigational Bacillus calmette-guerin substrain tice live antigen The risk or severity of adverse effects can be increased when Formestane is combined with Bacillus calmette-guerin substrain tice live antigen. Approved Balsalazide The risk or severity of adverse effects can be increased when Balsalazide is combined with Formestane. Approved, Investigational BCG vaccine The risk or severity of adverse effects can be increased when Formestane is combined with BCG vaccine. Investigational Bendazac The risk or severity of adverse effects can be increased when Bendazac is combined with Formestane. Experimental Bendroflumethiazide Formestane may increase the hypokalemic activities of Bendroflumethiazide. Approved Benorilate The risk or severity of adverse effects can be increased when Benorilate is combined with Formestane. Experimental Benoxaprofen The risk or severity of adverse effects can be increased when Benoxaprofen is combined with Formestane. Withdrawn Benzoic Acid The therapeutic efficacy of Benzoic Acid can be decreased when used in combination with Formestane. Approved, Investigational Benzydamine The risk or severity of adverse effects can be increased when Benzydamine is combined with Formestane. Approved Bevacizumab Bevacizumab may increase the cardiotoxic activities of Formestane. Approved, Investigational Bevonium The risk or severity of adverse effects can be increased when Bevonium is combined with Formestane. Experimental Bismuth Subcitrate The bioavailability of Formestane can be decreased when combined with Bismuth Subcitrate. Approved, Investigational Bismuth subnitrate The bioavailability of Formestane can be decreased when combined with Bismuth subnitrate. Approved, Experimental Boceprevir The serum concentration of Formestane can be increased when it is combined with Boceprevir. Approved, Withdrawn Bromfenac The risk or severity of adverse effects can be increased when Bromfenac is combined with Formestane. Approved Bucillamine The risk or severity of adverse effects can be increased when Bucillamine is combined with Formestane. Investigational Bufexamac The risk or severity of adverse effects can be increased when Bufexamac is combined with Formestane. Approved, Experimental Bumadizone The risk or severity of adverse effects can be increased when Bumadizone is combined with Formestane. Experimental Bumetanide Formestane may increase the hypokalemic activities of Bumetanide. Approved Cabazitaxel The risk or severity of adverse effects can be increased when Cabazitaxel is combined with Formestane. Approved Calcitriol The therapeutic efficacy of Calcitriol can be decreased when used in combination with Formestane. Approved, Nutraceutical Calcium Carbonate The bioavailability of Formestane can be decreased when combined with Calcium Carbonate. Approved, Investigational Calcium silicate The bioavailability of Formestane can be decreased when combined with Calcium silicate. Experimental Capromab pendetide Formestane may decrease effectiveness of Capromab pendetide as a diagnostic agent. Approved Carbamazepine The serum concentration of Formestane can be decreased when it is combined with Carbamazepine. Approved, Investigational Carbaspirin calcium The risk or severity of adverse effects can be increased when Carbaspirin calcium is combined with Formestane. Experimental, Investigational Carprofen The risk or severity of adverse effects can be increased when Carprofen is combined with Formestane. Approved, Vet Approved, Withdrawn Castanospermine The risk or severity of adverse effects can be increased when Castanospermine is combined with Formestane. Experimental Celecoxib The risk or severity of adverse effects can be increased when Celecoxib is combined with Formestane. Approved, Investigational Ceritinib Formestane may increase the hyperglycemic activities of Ceritinib. Approved Chloroquine The risk or severity of adverse effects can be increased when Chloroquine is combined with Formestane. Approved, Investigational, Vet Approved Chlorothiazide Formestane may increase the hypokalemic activities of Chlorothiazide. Approved, Vet Approved Chlorotrianisene The serum concentration of Formestane can be increased when it is combined with Chlorotrianisene. Investigational, Withdrawn Chlorthalidone Formestane may increase the hypokalemic activities of Chlorthalidone. Approved Cholestyramine Cholestyramine can cause a decrease in the absorption of Formestane resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved, Investigational Choline magnesium trisalicylate The risk or severity of adverse effects can be increased when Choline magnesium trisalicylate is combined with Formestane. Approved Cinoxacin The risk or severity of adverse effects can be increased when Formestane is combined with Cinoxacin. Approved, Investigational, Withdrawn Clarithromycin The serum concentration of Formestane can be increased when it is combined with Clarithromycin. Approved Clonixin The risk or severity of adverse effects can be increased when Clonixin is combined with Formestane. Approved Clostridium tetani toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Formestane is combined with Clostridium tetani toxoid antigen (formaldehyde inactivated). Approved Cobicistat The serum concentration of Formestane can be increased when it is combined with Cobicistat. Approved Colesevelam Colesevelam can cause a decrease in the absorption of Formestane resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved Colestipol Colestipol can cause a decrease in the absorption of Formestane resulting in a reduced serum concentration and potentially a decrease in efficacy. Approved Conjugated estrogens The serum concentration of Formestane can be increased when it is combined with Conjugated estrogens. Approved Corticorelin ovine triflutate The therapeutic efficacy of Corticorelin ovine triflutate can be decreased when used in combination with Formestane. Approved Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Formestane is combined with Corynebacterium diphtheriae toxoid antigen (formaldehyde inactivated). Approved Coumaphos The risk or severity of adverse effects can be increased when Formestane is combined with Coumaphos. Vet Approved Curcumin The risk or severity of adverse effects can be increased when Curcumin is combined with Formestane. Approved, Investigational Cyclopenthiazide Formestane may increase the hypokalemic activities of Cyclopenthiazide. Experimental Cyclophosphamide Cyclophosphamide may increase the cardiotoxic activities of Formestane. Approved, Investigational Cymarin Cymarin may decrease the cardiotoxic activities of Formestane. Experimental Daidzein The serum concentration of Formestane can be increased when it is combined with Daidzein. Experimental Danazol Formestane may increase the fluid retaining activities of Danazol. Approved Darunavir The serum concentration of Formestane can be increased when it is combined with Darunavir. Approved Decamethonium The risk or severity of adverse effects can be increased when Formestane is combined with Decamethonium. Approved Deferasirox The risk or severity of adverse effects can be increased when Formestane is combined with Deferasirox. Approved, Investigational Demecarium The risk or severity of adverse effects can be increased when Formestane is combined with Demecarium. Approved Dersalazine The risk or severity of adverse effects can be increased when Dersalazine is combined with Formestane. Investigational Deslanoside Deslanoside may decrease the cardiotoxic activities of Formestane. Approved Dichlorvos The risk or severity of adverse effects can be increased when Formestane is combined with Dichlorvos. Vet Approved Diclofenac The risk or severity of adverse effects can be increased when Diclofenac is combined with Formestane. Approved, Vet Approved Dienestrol The serum concentration of Formestane can be increased when it is combined with Dienestrol. Approved, Investigational Diethylstilbestrol The serum concentration of Formestane can be increased when it is combined with Diethylstilbestrol. Approved, Investigational Difenpiramide The risk or severity of adverse effects can be increased when Difenpiramide is combined with Formestane. Experimental Diflunisal The risk or severity of adverse effects can be increased when Diflunisal is combined with Formestane. Approved, Investigational Digitoxin Digitoxin may decrease the cardiotoxic activities of Formestane. Approved, Investigational Digoxin Digoxin may decrease the cardiotoxic activities of Formestane. Approved Digoxin Immune Fab (Ovine) Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Formestane. Approved Distigmine The risk or severity of adverse effects can be increased when Formestane is combined with Distigmine. Experimental Docetaxel The risk or severity of adverse effects can be increased when Docetaxel is combined with Formestane. Approved, Investigational Donepezil The risk or severity of adverse effects can be increased when Formestane is combined with Donepezil. Approved Droxicam The risk or severity of adverse effects can be increased when Droxicam is combined with Formestane. Withdrawn Duvelisib The risk or severity of adverse effects can be increased when Duvelisib is combined with Formestane. Investigational E-6201 The risk or severity of adverse effects can be increased when E-6201 is combined with Formestane. Investigational Echothiophate The risk or severity of adverse effects can be increased when Formestane is combined with Echothiophate. Approved Edrophonium The risk or severity of adverse effects can be increased when Formestane is combined with Edrophonium. Approved Enoxacin The risk or severity of adverse effects can be increased when Formestane is combined with Enoxacin. Approved, Investigational Enzalutamide The serum concentration of Formestane can be decreased when it is combined with Enzalutamide. Approved Epimestrol The serum concentration of Formestane can be increased when it is combined with Epimestrol. Experimental Epirizole The risk or severity of adverse effects can be increased when Epirizole is combined with Formestane. Approved Epitizide Formestane may increase the hypokalemic activities of Epitizide. Experimental Equol The serum concentration of Formestane can be increased when it is combined with Equol. Investigational Estradiol The serum concentration of Formestane can be increased when it is combined with Estradiol. Approved, Investigational, Vet Approved Estradiol acetate The serum concentration of Formestane can be increased when it is combined with Estradiol acetate. Approved, Investigational, Vet Approved Estradiol cypionate The serum concentration of Formestane can be increased when it is combined with Estradiol cypionate. Approved, Investigational, Vet Approved Estradiol valerate The serum concentration of Formestane can be increased when it is combined with Estradiol valerate. Approved, Investigational, Vet Approved Estriol The serum concentration of Formestane can be increased when it is combined with Estriol. Approved, Investigational, Vet Approved Estrogens, esterified The serum concentration of Formestane can be increased when it is combined with Estrogens, esterified. Approved Estrone The serum concentration of Formestane can be increased when it is combined with Estrone. Approved Etacrynic acid Formestane may increase the hypokalemic activities of Etacrynic acid. Approved, Investigational Etanercept The risk or severity of adverse effects can be increased when Etanercept is combined with Formestane. Approved, Investigational Ethenzamide The risk or severity of adverse effects can be increased when Ethenzamide is combined with Formestane. Experimental Ethinyl Estradiol The serum concentration of Formestane can be increased when it is combined with Ethinyl Estradiol. Approved Etodolac The risk or severity of adverse effects can be increased when Etodolac is combined with Formestane. Approved, Investigational, Vet Approved Etofenamate The risk or severity of adverse effects can be increased when Etofenamate is combined with Formestane. Approved, Investigational Etoricoxib The risk or severity of adverse effects can be increased when Etoricoxib is combined with Formestane. Approved, Investigational Evening primrose oil The risk or severity of adverse effects can be increased when Evening primrose oil is combined with Formestane. Approved, Investigational Exisulind The risk or severity of adverse effects can be increased when Exisulind is combined with Formestane. Investigational Felbinac The risk or severity of adverse effects can be increased when Felbinac is combined with Formestane. Experimental Fenbufen The risk or severity of adverse effects can be increased when Fenbufen is combined with Formestane. Approved Fenoprofen The risk or severity of adverse effects can be increased when Fenoprofen is combined with Formestane. Approved Fenthion The risk or severity of adverse effects can be increased when Formestane is combined with Fenthion. Vet Approved Fentiazac The risk or severity of adverse effects can be increased when Fentiazac is combined with Formestane. Experimental Feprazone The risk or severity of adverse effects can be increased when Feprazone is combined with Formestane. Experimental Ferulic acid The risk or severity of adverse effects can be increased when Ferulic acid is combined with Formestane. Experimental Fleroxacin The risk or severity of adverse effects can be increased when Formestane is combined with Fleroxacin. Approved Floctafenine The risk or severity of adverse effects can be increased when Floctafenine is combined with Formestane. Approved, Withdrawn Flumequine The risk or severity of adverse effects can be increased when Formestane is combined with Flumequine. Withdrawn Flunixin The risk or severity of adverse effects can be increased when Flunixin is combined with Formestane. Vet Approved Flunoxaprofen The risk or severity of adverse effects can be increased when Flunoxaprofen is combined with Formestane. Experimental Fluoxymesterone Formestane may increase the fluid retaining activities of Fluoxymesterone. Approved, Illicit Flurbiprofen The risk or severity of adverse effects can be increased when Flurbiprofen is combined with Formestane. Approved, Investigational Fosaprepitant The serum concentration of Formestane can be increased when it is combined with Fosaprepitant. Approved Fosphenytoin The serum concentration of Formestane can be decreased when it is combined with Fosphenytoin. Approved, Investigational Furosemide Formestane may increase the hypokalemic activities of Furosemide. Approved, Vet Approved G17DT The risk or severity of adverse effects can be increased when Formestane is combined with G17DT. Investigational Galantamine The risk or severity of adverse effects can be increased when Formestane is combined with Galantamine. Approved Gallamine Triethiodide The risk or severity of adverse effects can be increased when Formestane is combined with Gallamine Triethiodide. Approved Garenoxacin The risk or severity of adverse effects can be increased when Formestane is combined with Garenoxacin. Investigational Gatifloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Gatifloxacin. Approved, Investigational Gemifloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Gemifloxacin. Approved, Investigational Genistein The serum concentration of Formestane can be increased when it is combined with Genistein. Investigational GI-5005 The risk or severity of adverse effects can be increased when Formestane is combined with GI-5005. Investigational Gitoformate Gitoformate may decrease the cardiotoxic activities of Formestane. Experimental GLPG-0492 Formestane may increase the fluid retaining activities of GLPG-0492. Investigational Glycerol Phenylbutyrate The therapeutic efficacy of Glycerol Phenylbutyrate can be decreased when used in combination with Formestane. Approved Grepafloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Grepafloxacin. Approved, Investigational, Withdrawn Guacetisal The risk or severity of adverse effects can be increased when Guacetisal is combined with Formestane. Experimental Hemoglobin crosfumaril The risk or severity of adverse effects can be increased when Hemoglobin crosfumaril is combined with Formestane. Experimental Hepatitis A Vaccine The risk or severity of adverse effects can be increased when Formestane is combined with Hepatitis A Vaccine. Approved Hepatitis B Vaccine (Recombinant) The risk or severity of adverse effects can be increased when Formestane is combined with Hepatitis B Vaccine (Recombinant). Approved, Withdrawn Hexestrol The serum concentration of Formestane can be increased when it is combined with Hexestrol. Withdrawn Higenamine The risk or severity of adverse effects can be increased when Higenamine is combined with Formestane. Investigational Human rabies virus immune globulin The risk or severity of adverse effects can be increased when Formestane is combined with Human rabies virus immune globulin. Approved Huperzine A The risk or severity of adverse effects can be increased when Formestane is combined with Huperzine A. Approved, Investigational Hyaluronidase The therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Formestane. Approved, Investigational Hydrochlorothiazide Formestane may increase the hypokalemic activities of Hydrochlorothiazide. Approved, Vet Approved Hydroflumethiazide Formestane may increase the hypokalemic activities of Hydroflumethiazide. Approved, Investigational Hydrotalcite The bioavailability of Formestane can be decreased when combined with Hydrotalcite. Approved, Experimental, Investigational Ibuprofen The risk or severity of adverse effects can be increased when Ibuprofen is combined with Formestane. Approved Ibuproxam The risk or severity of adverse effects can be increased when Ibuproxam is combined with Formestane. Withdrawn Icatibant The risk or severity of adverse effects can be increased when Icatibant is combined with Formestane. Approved, Investigational Idelalisib The serum concentration of Formestane can be increased when it is combined with Idelalisib. Approved Imidazole salicylate The risk or severity of adverse effects can be increased when Imidazole salicylate is combined with Formestane. Experimental Indacaterol Indacaterol may increase the hypokalemic activities of Formestane. Approved Indapamide Formestane may increase the hypokalemic activities of Indapamide. Approved Indinavir The serum concentration of Formestane can be increased when it is combined with Indinavir. Approved Indobufen The risk or severity of adverse effects can be increased when Indobufen is combined with Formestane. Investigational Indomethacin The risk or severity of adverse effects can be increased when Indomethacin is combined with Formestane. Approved, Investigational Indoprofen The risk or severity of adverse effects can be increased when Indoprofen is combined with Formestane. Withdrawn INGN 201 The risk or severity of adverse effects can be increased when Formestane is combined with INGN 201. Investigational INGN 225 The risk or severity of adverse effects can be increased when Formestane is combined with INGN 225. Investigational Ipidacrine The risk or severity of adverse effects can be increased when Formestane is combined with Ipidacrine. Experimental Isoflurophate The risk or severity of adverse effects can be increased when Formestane is combined with Isoflurophate. Approved, Investigational, Withdrawn Isoniazid The serum concentration of Isoniazid can be decreased when it is combined with Formestane. Approved, Investigational Isoxicam The risk or severity of adverse effects can be increased when Isoxicam is combined with Formestane. Withdrawn Itraconazole The serum concentration of Formestane can be increased when it is combined with Itraconazole. Approved, Investigational Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated) The risk or severity of adverse effects can be increased when Formestane is combined with Japanese encephalitis virus strain sa 14-14-2 antigen (formaldehyde inactivated). Approved Kebuzone The risk or severity of adverse effects can be increased when Kebuzone is combined with Formestane. Experimental Ketoconazole The serum concentration of Formestane can be increased when it is combined with Ketoconazole. Approved, Investigational Ketoprofen The risk or severity of adverse effects can be increased when Ketoprofen is combined with Formestane. Approved, Vet Approved Ketorolac The risk or severity of adverse effects can be increased when Ketorolac is combined with Formestane. Approved Lacidipine The serum concentration of Lacidipine can be decreased when it is combined with Formestane. Approved, Investigational Lanatoside C Lanatoside C may decrease the cardiotoxic activities of Formestane. Experimental Leflunomide The risk or severity of adverse effects can be increased when Leflunomide is combined with Formestane. Approved, Investigational Levofloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Levofloxacin. Approved, Investigational Lisofylline The risk or severity of adverse effects can be increased when Lisofylline is combined with Formestane. Investigational Lonazolac The risk or severity of adverse effects can be increased when Lonazolac is combined with Formestane. Experimental Lopinavir The serum concentration of Formestane can be increased when it is combined with Lopinavir. Approved Lornoxicam The risk or severity of adverse effects can be increased when Lornoxicam is combined with Formestane. Approved, Investigational Loxoprofen The risk or severity of adverse effects can be increased when Loxoprofen is combined with Formestane. Approved, Investigational Lumacaftor The serum concentration of Formestane can be decreased when it is combined with Lumacaftor. Approved Lumiracoxib The risk or severity of adverse effects can be increased when Lumiracoxib is combined with Formestane. Approved, Investigational Magaldrate The bioavailability of Formestane can be decreased when combined with Magaldrate. Approved, Withdrawn Magnesium hydroxide The bioavailability of Formestane can be decreased when combined with Magnesium hydroxide. Approved, Investigational Magnesium oxide The bioavailability of Formestane can be decreased when combined with Magnesium oxide. Approved Magnesium peroxide The bioavailability of Formestane can be decreased when combined with Magnesium peroxide. Experimental Magnesium salicylate The risk or severity of adverse effects can be increased when Magnesium salicylate is combined with Formestane. Approved Magnesium silicate The bioavailability of Formestane can be decreased when combined with Magnesium silicate. Approved Magnesium Trisilicate The bioavailability of Formestane can be decreased when combined with Magnesium Trisilicate. Approved Malathion The risk or severity of adverse effects can be increased when Formestane is combined with Malathion. Approved, Investigational Masoprocol The risk or severity of adverse effects can be increased when Masoprocol is combined with Formestane. Approved, Investigational Meclofenamic acid The risk or severity of adverse effects can be increased when Meclofenamic acid is combined with Formestane. Approved, Vet Approved Mefenamic acid The risk or severity of adverse effects can be increased when Mefenamic acid is combined with Formestane. Approved Mefloquine The risk or severity of adverse effects can be increased when Formestane is combined with Mefloquine. Approved, Investigational Meloxicam The risk or severity of adverse effects can be increased when Meloxicam is combined with Formestane. Approved, Vet Approved Memantine The risk or severity of adverse effects can be increased when Formestane is combined with Memantine. Approved, Investigational Mesalazine The risk or severity of adverse effects can be increased when Mesalazine is combined with Formestane. Approved Mesterolone Formestane may increase the fluid retaining activities of Mesterolone. Experimental Mestranol The serum concentration of Formestane can be increased when it is combined with Mestranol. Approved Metamizole The risk or severity of adverse effects can be increased when Metamizole is combined with Formestane. Approved, Investigational, Withdrawn Methadone The serum concentration of Methadone can be increased when it is combined with Formestane. Approved Methallenestril The serum concentration of Formestane can be increased when it is combined with Methallenestril. Experimental Methanesulfonyl Fluoride The risk or severity of adverse effects can be increased when Formestane is combined with Methanesulfonyl Fluoride. Investigational Methyclothiazide Formestane may increase the hypokalemic activities of Methyclothiazide. Approved Methyl salicylate The risk or severity of adverse effects can be increased when Methyl salicylate is combined with Formestane. Approved, Vet Approved Methyltestosterone Formestane may increase the fluid retaining activities of Methyltestosterone. Approved Metildigoxin Metildigoxin may decrease the cardiotoxic activities of Formestane. Experimental Metoclopramide The risk or severity of adverse effects can be increased when Formestane is combined with Metoclopramide. Approved, Investigational Metolazone Formestane may increase the hypokalemic activities of Metolazone. Approved Mifepristone The therapeutic efficacy of Formestane can be decreased when used in combination with Mifepristone. Approved, Investigational Minaprine The risk or severity of adverse effects can be increased when Formestane is combined with Minaprine. Approved Mitotane The serum concentration of Formestane can be decreased when it is combined with Mitotane. Approved Mivacurium Mivacurium may increase the adverse neuromuscular activities of Formestane. Approved Mizoribine The risk or severity of adverse effects can be increased when Mizoribine is combined with Formestane. Investigational Mofebutazone The risk or severity of adverse effects can be increased when Mofebutazone is combined with Formestane. Experimental Moxestrol The serum concentration of Formestane can be increased when it is combined with Moxestrol. Experimental Mycophenolate mofetil The risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Formestane. Approved, Investigational Mycophenolic acid The risk or severity of adverse effects can be increased when Mycophenolic acid is combined with Formestane. Approved Nabumetone The risk or severity of adverse effects can be increased when Nabumetone is combined with Formestane. Approved Nafamostat The risk or severity of adverse effects can be increased when Nafamostat is combined with Formestane. Approved, Investigational Naftifine The risk or severity of adverse effects can be increased when Naftifine is combined with Formestane. Approved Nalidixic Acid The risk or severity of adverse effects can be increased when Formestane is combined with Nalidixic Acid. Approved, Investigational Nandrolone Formestane may increase the fluid retaining activities of Nandrolone. Experimental, Investigational Nandrolone decanoate Formestane may increase the fluid retaining activities of Nandrolone decanoate. Approved, Illicit Naproxen The risk or severity of adverse effects can be increased when Naproxen is combined with Formestane. Approved, Vet Approved Nefazodone The serum concentration of Formestane can be increased when it is combined with Nefazodone. Approved, Withdrawn Nelfinavir The serum concentration of Formestane can be increased when it is combined with Nelfinavir. Approved Nemonoxacin The risk or severity of adverse effects can be increased when Formestane is combined with Nemonoxacin. Investigational Neostigmine The risk or severity of adverse effects can be increased when Formestane is combined with Neostigmine. Approved, Vet Approved Nepafenac The risk or severity of adverse effects can be increased when Nepafenac is combined with Formestane. Approved, Investigational Nevirapine The serum concentration of Formestane can be decreased when it is combined with Nevirapine. Approved Nicorandil The risk or severity of adverse effects can be increased when Formestane is combined with Nicorandil. Approved, Investigational Nifenazone The risk or severity of adverse effects can be increased when Nifenazone is combined with Formestane. Experimental Niflumic Acid The risk or severity of adverse effects can be increased when Niflumic Acid is combined with Formestane. Approved Nimesulide The risk or severity of adverse effects can be increased when Nimesulide is combined with Formestane. Approved, Investigational, Withdrawn Nitroaspirin The risk or severity of adverse effects can be increased when Nitroaspirin is combined with Formestane. Investigational Norfloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Norfloxacin. Approved Oleandrin Oleandrin may decrease the cardiotoxic activities of Formestane. Experimental, Investigational Olopatadine The risk or severity of adverse effects can be increased when Olopatadine is combined with Formestane. Approved Olsalazine The risk or severity of adverse effects can be increased when Olsalazine is combined with Formestane. Approved Orgotein The risk or severity of adverse effects can be increased when Orgotein is combined with Formestane. Vet Approved Ouabain Ouabain may decrease the cardiotoxic activities of Formestane. Approved Oxandrolone Formestane may increase the fluid retaining activities of Oxandrolone. Approved, Investigational Oxaprozin The risk or severity of adverse effects can be increased when Oxaprozin is combined with Formestane. Approved Oxolinic acid The risk or severity of adverse effects can be increased when Formestane is combined with Oxolinic acid. Experimental Oxymetholone Formestane may increase the fluid retaining activities of Oxymetholone. Approved, Illicit Oxyphenbutazone The risk or severity of adverse effects can be increased when Oxyphenbutazone is combined with Formestane. Approved, Withdrawn Paclitaxel The risk or severity of adverse effects can be increased when Paclitaxel is combined with Formestane. Approved, Vet Approved Paraoxon The risk or severity of adverse effects can be increased when Formestane is combined with Paraoxon. Experimental Parecoxib The risk or severity of adverse effects can be increased when Parecoxib is combined with Formestane. Approved Parthenolide The risk or severity of adverse effects can be increased when Parthenolide is combined with Formestane. Approved, Investigational Pazufloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Pazufloxacin. Investigational Pefloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Pefloxacin. Approved Pentobarbital The serum concentration of Formestane can be decreased when it is combined with Pentobarbital. Approved, Investigational, Vet Approved Peruvoside Peruvoside may decrease the cardiotoxic activities of Formestane. Experimental Phenobarbital The serum concentration of Formestane can be decreased when it is combined with Phenobarbital. Approved, Investigational Phenyl aminosalicylate The risk or severity of adverse effects can be increased when Phenyl aminosalicylate is combined with Formestane. Approved Phenylacetic acid The therapeutic efficacy of Phenylacetic acid can be decreased when used in combination with Formestane. Approved Phenylbutazone The risk or severity of adverse effects can be increased when Phenylbutazone is combined with Formestane. Approved, Vet Approved Phenylbutyric acid The therapeutic efficacy of Phenylbutyric acid can be decreased when used in combination with Formestane. Approved, Investigational Phenytoin The serum concentration of Formestane can be decreased when it is combined with Phenytoin. Approved, Vet Approved Physostigmine The risk or severity of adverse effects can be increased when Formestane is combined with Physostigmine. Approved, Investigational Pimecrolimus The risk or severity of adverse effects can be increased when Pimecrolimus is combined with Formestane. Approved, Investigational Pipemidic acid The risk or severity of adverse effects can be increased when Formestane is combined with Pipemidic acid. Experimental Piretanide Formestane may increase the hypokalemic activities of Piretanide. Approved Pirfenidone The risk or severity of adverse effects can be increased when Pirfenidone is combined with Formestane. Approved, Investigational Piromidic acid The risk or severity of adverse effects can be increased when Formestane is combined with Piromidic acid. Experimental Piroxicam The risk or severity of adverse effects can be increased when Piroxicam is combined with Formestane. Approved, Investigational Pirprofen The risk or severity of adverse effects can be increased when Pirprofen is combined with Formestane. Experimental Polyestradiol phosphate The serum concentration of Formestane can be increased when it is combined with Polyestradiol phosphate. Approved Polythiazide Formestane may increase the hypokalemic activities of Polythiazide. Approved Posaconazole The serum concentration of Formestane can be increased when it is combined with Posaconazole. Approved, Investigational, Vet Approved Pranoprofen The risk or severity of adverse effects can be increased when Pranoprofen is combined with Formestane. Experimental, Investigational Primidone The serum concentration of Formestane can be decreased when it is combined with Primidone. Approved, Vet Approved Proglumetacin The risk or severity of adverse effects can be increased when Proglumetacin is combined with Formestane. Experimental Promestriene The serum concentration of Formestane can be increased when it is combined with Promestriene. Investigational Propacetamol The risk or severity of adverse effects can be increased when Propacetamol is combined with Formestane. Approved, Investigational Propyphenazone The risk or severity of adverse effects can be increased when Propyphenazone is combined with Formestane. Experimental Proquazone The risk or severity of adverse effects can be increased when Proquazone is combined with Formestane. Experimental Proscillaridin Proscillaridin may decrease the cardiotoxic activities of Formestane. Experimental Prulifloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Prulifloxacin. Investigational PTC299 The risk or severity of adverse effects can be increased when PTC299 is combined with Formestane. Investigational Pyridostigmine The risk or severity of adverse effects can be increased when Formestane is combined with Pyridostigmine. Approved, Investigational Quinestrol The serum concentration of Formestane can be increased when it is combined with Quinestrol. Approved Quinethazone Formestane may increase the hypokalemic activities of Quinethazone. Approved Rabies virus inactivated antigen, A The risk or severity of adverse effects can be increased when Formestane is combined with Rabies virus inactivated antigen, A. Approved, Investigational Rapacuronium Rapacuronium may increase the adverse neuromuscular activities of Formestane. Withdrawn Resveratrol The risk or severity of adverse effects can be increased when Resveratrol is combined with Formestane. Approved, Experimental, Investigational Rifabutin The serum concentration of Formestane can be decreased when it is combined with Rifabutin. Approved, Investigational Rifampicin The serum concentration of Formestane can be decreased when it is combined with Rifampicin. Approved Rifapentine The serum concentration of Formestane can be decreased when it is combined with Rifapentine. Approved, Investigational Rindopepimut The risk or severity of adverse effects can be increased when Formestane is combined with Rindopepimut. Investigational Rivastigmine The risk or severity of adverse effects can be increased when Formestane is combined with Rivastigmine. Approved, Investigational Rofecoxib The risk or severity of adverse effects can be increased when Rofecoxib is combined with Formestane. Approved, Investigational, Withdrawn Rosoxacin The risk or severity of adverse effects can be increased when Formestane is combined with Rosoxacin. Approved, Investigational Rotavirus Vaccine The risk or severity of adverse effects can be increased when Formestane is combined with Rotavirus Vaccine. Approved Rubella virus vaccine The risk or severity of adverse effects can be increased when Formestane is combined with Rubella virus vaccine. Approved, Investigational Rufloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Rufloxacin. Experimental Salicylamide The risk or severity of adverse effects can be increased when Salicylamide is combined with Formestane. Approved Salicylic acid The risk or severity of adverse effects can be increased when Salicylic acid is combined with Formestane. Approved, Investigational, Vet Approved Salmonella typhi ty2 vi polysaccharide antigen The risk or severity of adverse effects can be increased when Formestane is combined with Salmonella typhi ty2 vi polysaccharide antigen. Approved Salmonella typhi ty21a live antigen The risk or severity of adverse effects can be increased when Formestane is combined with Salmonella typhi ty21a live antigen. Approved Salsalate The risk or severity of adverse effects can be increased when Salsalate is combined with Formestane. Approved Saquinavir The serum concentration of Formestane can be increased when it is combined with Saquinavir. Approved, Investigational Secoisolariciresinol The serum concentration of Formestane can be increased when it is combined with Secoisolariciresinol. Investigational Semapimod The risk or severity of adverse effects can be increased when Semapimod is combined with Formestane. Investigational Seratrodast The risk or severity of adverse effects can be increased when Seratrodast is combined with Formestane. Approved Serrapeptase The risk or severity of adverse effects can be increased when Serrapeptase is combined with Formestane. Investigational Sitafloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Sitafloxacin. Experimental, Investigational Sodium bicarbonate The bioavailability of Formestane can be decreased when combined with Sodium bicarbonate. Approved Sparfloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Sparfloxacin. Approved, Investigational SRP 299 The risk or severity of adverse effects can be increased when Formestane is combined with SRP 299. Investigational SRT501 The risk or severity of adverse effects can be increased when SRT501 is combined with Formestane. Investigational St. John's Wort The serum concentration of Formestane can be decreased when it is combined with St. John's Wort. Approved, Investigational, Nutraceutical Stanolone Formestane may increase the fluid retaining activities of Stanolone. Illicit, Investigational Stanozolol Formestane may increase the fluid retaining activities of Stanozolol. Approved, Vet Approved Stiripentol The serum concentration of Formestane can be increased when it is combined with Stiripentol. Approved Sulfasalazine The risk or severity of adverse effects can be increased when Sulfasalazine is combined with Formestane. Approved Sulindac The risk or severity of adverse effects can be increased when Sulindac is combined with Formestane. Approved, Investigational Suprofen The risk or severity of adverse effects can be increased when Suprofen is combined with Formestane. Approved, Withdrawn Suxibuzone The risk or severity of adverse effects can be increased when Suxibuzone is combined with Formestane. Experimental Synthetic Conjugated Estrogens, A The serum concentration of Formestane can be increased when it is combined with Synthetic Conjugated Estrogens, A. Approved Synthetic Conjugated Estrogens, B The serum concentration of Formestane can be increased when it is combined with Synthetic Conjugated Estrogens, B. Approved Tacrine The risk or severity of adverse effects can be increased when Formestane is combined with Tacrine. Investigational, Withdrawn Tarenflurbil The risk or severity of adverse effects can be increased when Tarenflurbil is combined with Formestane. Investigational Tecemotide The risk or severity of adverse effects can be increased when Formestane is combined with Tecemotide. Investigational Telaprevir The serum concentration of Telaprevir can be decreased when it is combined with Formestane. Approved, Withdrawn Telithromycin The serum concentration of Formestane can be increased when it is combined with Telithromycin. Approved Temafloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Temafloxacin. Withdrawn Tenidap The risk or severity of adverse effects can be increased when Tenidap is combined with Formestane. Experimental Tenoxicam The risk or severity of adverse effects can be increased when Tenoxicam is combined with Formestane. Approved Tepoxalin The risk or severity of adverse effects can be increased when Tepoxalin is combined with Formestane. Vet Approved Teriflunomide The risk or severity of adverse effects can be increased when Teriflunomide is combined with Formestane. Approved Testosterone Formestane may increase the fluid retaining activities of Testosterone. Approved, Investigational Testosterone cypionate Formestane may increase the fluid retaining activities of Testosterone cypionate. Approved Testosterone enanthate Formestane may increase the fluid retaining activities of Testosterone enanthate. Approved Testosterone propionate Formestane may increase the fluid retaining activities of Testosterone propionate. Approved, Investigational, Vet Approved, Withdrawn Testosterone undecanoate Formestane may increase the fluid retaining activities of Testosterone undecanoate. Approved, Investigational TG4010 The risk or severity of adverse effects can be increased when Formestane is combined with TG4010. Investigational Tiaprofenic acid The risk or severity of adverse effects can be increased when Tiaprofenic acid is combined with Formestane. Approved Tibolone The serum concentration of Formestane can be increased when it is combined with Tibolone. Approved, Investigational Tinoridine The risk or severity of adverse effects can be increased when Tinoridine is combined with Formestane. Investigational Tolfenamic Acid The risk or severity of adverse effects can be increased when Tolfenamic Acid is combined with Formestane. Approved, Investigational Tolmetin The risk or severity of adverse effects can be increased when Tolmetin is combined with Formestane. Approved Torasemide Formestane may increase the hypokalemic activities of Torasemide. Approved Tranilast The risk or severity of adverse effects can be increased when Tranilast is combined with Formestane. Approved, Investigational Trastuzumab Trastuzumab may increase the cardiotoxic activities of Formestane. Approved, Investigational Tribenoside The risk or severity of adverse effects can be increased when Tribenoside is combined with Formestane. Experimental Trichlorfon The risk or severity of adverse effects can be increased when Formestane is combined with Trichlorfon. Vet Approved Trichlormethiazide Formestane may increase the hypokalemic activities of Trichlormethiazide. Approved, Vet Approved Triptolide The risk or severity of adverse effects can be increased when Triptolide is combined with Formestane. Investigational Trolamine salicylate The risk or severity of adverse effects can be increased when Trolamine salicylate is combined with Formestane. Approved Tromethamine The bioavailability of Formestane can be decreased when combined with Tromethamine. Approved Trovafloxacin The risk or severity of adverse effects can be increased when Formestane is combined with Trovafloxacin. Approved, Investigational, Withdrawn Tubocurarine The risk or severity of adverse effects can be increased when Formestane is combined with Tubocurarine. Approved Valdecoxib The risk or severity of adverse effects can be increased when Valdecoxib is combined with Formestane. Approved, Investigational, Withdrawn Varicella Zoster Vaccine (Live/Attenuated) The risk or severity of adverse effects can be increased when Formestane is combined with Varicella Zoster Vaccine (Live/Attenuated). Approved Voriconazole The serum concentration of Formestane can be increased when it is combined with Voriconazole. Approved, Investigational Warfarin Formestane may increase the anticoagulant activities of Warfarin. Approved Yellow Fever Vaccine The risk or severity of adverse effects can be increased when Formestane is combined with Yellow Fever Vaccine. Approved, Investigational Zaltoprofen The risk or severity of adverse effects can be increased when Zaltoprofen is combined with Formestane. Approved, Investigational Zeranol The serum concentration of Formestane can be increased when it is combined with Zeranol. Vet Approved Zileuton The risk or severity of adverse effects can be increased when Zileuton is combined with Formestane. Approved, Investigational, Withdrawn Zomepirac The risk or severity of adverse effects can be increased when Zomepirac is combined with Formestane. Withdrawn - Food Interactions
- Not Available
References
- Synthesis Reference
Kohler, Maxie, et al. "Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites." Steroids 72.3 (2007): 278-286.
- General References
- Perez Carrion R, Alberola Candel V, Calabresi F, Michel RT, Santos R, Delozier T, Goss P, Mauriac L, Feuilhade F, Freue M, et al.: Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer. Ann Oncol. 1994;5 Suppl 7:S19-24. [PubMed:7873457]
- Kohler M, Parr MK, Opfermann G, Thevis M, Schlorer N, Marner FJ, Schanzer W: Metabolism of 4-hydroxyandrostenedione and 4-hydroxytestosterone: Mass spectrometric identification of urinary metabolites. Steroids. 2007 Mar;72(3):278-86. Epub 2007 Jan 17. [PubMed:17207827]
- Lonning PE, Geisler J, Johannessen DC, Gschwind HP, Waldmeier F, Schneider W, Galli B, Winkler T, Blum W, Kriemler HP, Miller WR, Faigle JW: Pharmacokinetics and metabolism of formestane in breast cancer patients. J Steroid Biochem Mol Biol. 2001 Apr;77(1):39-47. [PubMed:11358673]
- Murray R, Pitt P: Treatment of advanced breast cancer with formestane. Ann Oncol. 1994;5 Suppl 7:S11-3. [PubMed:7873455]
- Vorobiof DA, Kleeberg UR, Perez-Carrion R, Dodwell DJ, Robertson JF, Calvo L, Dowsett M, Clack G: A randomized, open, parallel-group trial to compare the endocrine effects of oral anastrozole (Arimidex) with intramuscular formestane in postmenopausal women with advanced breast cancer. Ann Oncol. 1999 Oct;10(10):1219-25. [PubMed:10586340]
- External Links
- KEGG Drug
- D07260
- PubChem Compound
- 11273
- PubChem Substance
- 175427144
- ChemSpider
- 10799
- BindingDB
- 225704
- ChEBI
- 75172
- ChEMBL
- CHEMBL132530
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Formestane
- ATC Codes
- L02BG02 — Formestane
- MSDS
- Download (279 KB)
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage forms
Form Route Strength Liquid; powder, for solution Intramuscular - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 199 - 202 MSDS water solubility Insoluble MSDS logP 2.66 MSDS pKa 9.31 MSDS - Predicted Properties
Property Value Source Water Solubility 0.0578 mg/mL ALOGPS logP 2.57 ALOGPS logP 3.41 ChemAxon logS -3.7 ALOGPS pKa (Strongest Acidic) 9.21 ChemAxon pKa (Strongest Basic) -3.7 ChemAxon Physiological Charge 0 ChemAxon Hydrogen Acceptor Count 3 ChemAxon Hydrogen Donor Count 1 ChemAxon Polar Surface Area 54.37 Å2 ChemAxon Rotatable Bond Count 0 ChemAxon Refractivity 85.57 m3·mol-1 ChemAxon Polarizability 34.07 Å3 ChemAxon Number of Rings 4 ChemAxon Bioavailability 1 ChemAxon Rule of Five Yes ChemAxon Ghose Filter Yes ChemAxon Veber's Rule No ChemAxon MDDR-like Rule No ChemAxon - Predicted ADMET features
Property Value Probability Human Intestinal Absorption + 1.0 Blood Brain Barrier + 0.9628 Caco-2 permeable + 0.8149 P-glycoprotein substrate Substrate 0.6597 P-glycoprotein inhibitor I Inhibitor 0.7113 P-glycoprotein inhibitor II Non-inhibitor 0.8526 Renal organic cation transporter Non-inhibitor 0.7227 CYP450 2C9 substrate Non-substrate 0.8331 CYP450 2D6 substrate Non-substrate 0.9308 CYP450 3A4 substrate Substrate 0.753 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9443 CYP450 2D6 inhibitor Non-inhibitor 0.941 CYP450 2C19 inhibitor Non-inhibitor 0.9025 CYP450 3A4 inhibitor Non-inhibitor 0.85 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.9027 Ames test Non AMES toxic 0.9311 Carcinogenicity Non-carcinogens 0.9537 Biodegradation Not ready biodegradable 0.963 Rat acute toxicity 1.6135 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9479 hERG inhibition (predictor II) Non-inhibitor 0.7566
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS Not Available Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS Not Available MS/MS Spectrum - , positive LC-MS/MS splash10-01t9-2920000000-24696d73561fe3ce6680
Taxonomy
- Description
- This compound belongs to the class of organic compounds known as androgens and derivatives. These are 3-hydroxylated C19 steroid hormones. They are known to favor the development of masculine characteristics. They also show profound effects on scalp and body hair in humans.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Androstane steroids
- Direct Parent
- Androgens and derivatives
- Alternative Parents
- Hydroxysteroids / 3-oxo delta-4-steroids / 17-oxosteroids / Delta-4-steroids / Cyclohexenones / Enols / Organic oxides / Hydrocarbon derivatives
- Substituents
- Androgen-skeleton / 3-oxo-delta-4-steroid / 3-oxosteroid / Oxosteroid / 17-oxosteroid / 4-hydroxysteroid / Hydroxysteroid / Delta-4-steroid / Cyclohexenone / Cyclic ketone
- Molecular Framework
- Aliphatic homopolycyclic compounds
- External Descriptors
- enol, 3-oxo Delta(4)-steroid, 17-oxo steroid, hydroxy steroid (CHEBI:75172)
Drug created on June 13, 2013 22:20 / Updated on March 02, 2018 03:43