You are using an unsupported browser. Please upgrade your browser to a newer version to get the best experience on DrugBank.
Identification
NameMegestrol acetate
Accession NumberDB00351  (APRD01092)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description17-Hydroxy-6-methylpregna-3,6-diene-3,20-dione. A progestational hormone used most commonly as the acetate ester. As the acetate, it is more potent than progesterone both as a progestagen and as an ovulation inhibitor. It has also been used in the palliative treatment of breast cancer.
Structure
Thumb
Synonyms
17-Acetoxy-6-methylpregna-4,6-diene-3,20-dione
17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate
17alpha-Acetoxy-6-dehydro-6-methylprogesterone
17alpha-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
17α-Acetoxy-6-dehydro-6-methylprogesterone
17α-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
6-Dehydro-6-methyl-17alpha-acetoxyprogesterone
6-Dehydro-6-methyl-17α-acetoxyprogesterone
6-Methyl-17alpha-acetoxypregna-4,6-diene-3,20-dione
6-Methyl-17alpha-hydroxy-delta(sup 6)-progesterone acetate
6-Methyl-17α-acetoxypregna-4,6-diene-3,20-dione
6-Methyl-17α-hydroxy-delta(sup 6)-progesterone acetate
6-Methyl-6-dehydro-17alpha-acetoxyprogesterone
6-Methyl-6-dehydro-17α-acetoxyprogesterone
6-Methyl-delta(sup 4,6)-pregnadien-17alpha-ol-3,20-dione acetate
6-Methyl-delta(sup 4,6)-pregnadien-17α-ol-3,20-dione acetate
6-Methyl-delta(sup 6)-dehydro-17alpha-acetoxyprogesterone
6-Methyl-delta(sup 6)-dehydro-17α-acetoxyprogesterone
MGA
External Identifiers
  • BDH 1298
  • BDH-1298
  • NSC-71423
  • SC 10363
  • SC-10363
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Linmegestrol - Tab 160mgTablet160 mgOralLinson Pharma Co.1995-12-312006-05-29Canada
Linmegestrol - Tab 40mgTablet40 mgOralLinson Pharma Co.1995-12-312004-08-05Canada
MegaceTablet160 mgOralBristol Myers Squibb Canada1987-12-312009-03-09Canada
MegaceSuspension40 mg/mLOralE.R. Squibb & Sons, L.L.C.2009-06-01Not applicableUs
MegaceTablet40 mgOralBristol Myers Squibb Canada1977-12-312006-05-29Canada
Megace EsSuspension125 mg/mLOralStat Rx USA2005-06-08Not applicableUs
Megace EsSuspension125 mg/mLOralPhysicians Total Care, Inc.2006-04-13Not applicableUs
Megace EsSuspension125 mg/mLOralAtlantic Biologicals Corps2005-07-02Not applicableUs
Megace EsSuspension125 mg/mLOralPar Pharmaceutical, Inc2005-07-02Not applicableUs
Megace OsSuspension40 mgOralBristol Myers Squibb Canada1995-12-31Not applicableCanada
MegestrolTablet40 mgOralAa Pharma Inc1995-12-31Not applicableCanada
MegestrolTablet160 mgOralAa Pharma Inc1995-12-31Not applicableCanada
Megestrol AcetateSuspension125 mg/mLOralPar Pharmaceutical, Inc.2015-07-28Not applicableUs
Megestrol-160 - Tab 160 mgTablet160 mgOralPro Doc Limitee1997-02-272010-07-13Canada
Megestrol-40 - Tab 40mgTablet40 mgOralPro Doc Limitee1997-02-272010-07-13Canada
Nu-megestrol - Tab 160mgTablet160 mgOralNu Pharm Inc1996-12-312012-09-04Canada
Nu-megestrol - Tab 40mgTablet40 mgOralNu Pharm Inc1996-12-312012-09-04Canada
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-megestrolTablet160 mgOralApotex IncNot applicableNot applicableCanada
Apo-megestrolTablet40 mgOralApotex IncNot applicableNot applicableCanada
MegestolSuspension40 mg/mLOralSTAT Rx USA LLC2002-02-15Not applicableUs
Megestrol AcetateTablet40 mg/1OralGolden State Medical Supply, Inc.2015-09-04Not applicableUs
Megestrol AcetateTablet40 mg/1OralWest Ward Pharmaceuticals Corp.1995-09-29Not applicableUs
Megestrol AcetateTablet20 mg/1OralPar Pharmaceutical Inc1988-08-08Not applicableUs
Megestrol AcetateTablet40 mg/1OralCardinal Health1995-11-30Not applicableUs
Megestrol AcetateSuspension400 mg/10mLOralPrecision Dose Inc.2004-02-252016-03-17Us
Megestrol AcetateSuspension40 mg/mLOralPharmaceutical Associates, Inc.2006-07-07Not applicableUs
Megestrol AcetateTablet40 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralVista Pharm, Inc.2012-08-22Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralRxchange Co2001-07-25Not applicableUs
Megestrol AcetateTablet40 mg/1OralMajor Pharmaceuticals2004-02-16Not applicableUs
Megestrol AcetateTablet20 mg/1OralCardinal Health2011-05-13Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralMorton Grove Pharmaceuticals, Inc.2005-02-09Not applicableUs
Megestrol AcetateTablet20 mg/1OralWest Ward Pharmaceuticals Corp.1995-09-29Not applicableUs
Megestrol AcetateTablet40 mg/1OralPar Pharmaceutical Inc1988-08-08Not applicableUs
Megestrol AcetateSuspension400 mg/10mLOralCardinal Health2004-02-25Not applicableUs
Megestrol AcetateTablet40 mg/1OralAvera Mc Kennan Hospital2015-03-02Not applicableUs
Megestrol AcetateTablet20 mg/1OralBarr Laboratories Inc.1996-10-25Not applicableUs
Megestrol AcetateSuspension125 mg/mLOralAv Kare, Inc.2016-06-09Not applicableUs
Megestrol AcetateTablet40 mg/1OralPhysicians Total Care, Inc.2007-07-05Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralPrecision Dose Inc.2014-06-23Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralWest Ward Pharmaceuticals Corp.2002-02-15Not applicableUs
Megestrol AcetateTablet40 mg/1OralCardinal Health2011-05-13Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralPar Pharmaceutical, Inc.2001-07-25Not applicableUs
Megestrol AcetateTablet40 mg/1OralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2007-08-20Not applicableUs
Megestrol AcetateTablet40 mg/1OralWest Ward Pharmaceuticals Corp.1995-09-29Not applicableUs
Megestrol AcetateTablet40 mg/1OralBarr Laboratories Inc.1995-11-30Not applicableUs
Megestrol AcetateSuspension400 mg/10mLOralCardinal Health2004-02-25Not applicableUs
Megestrol AcetateTablet40 mg/1OralUDL Laboratories, Inc.2011-05-132015-12-29Us
Megestrol AcetateSuspension40 mg/mLOralPrecision Dose Inc.2014-10-08Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralPhysicians Total Care, Inc.2005-09-01Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralCardinal Health2006-07-07Not applicableUs
Megestrol AcetateTablet20 mg/1OralWest Ward Pharmaceuticals Corp.1995-09-29Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralAtlantic Biologicals Corps2001-07-25Not applicableUs
Megestrol AcetateTablet20 mg/1OralMylan Institutional Inc.1997-08-07Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2013-03-08Not applicableUs
Megestrol AcetateSuspension125 mg/mLOralT Wi Pharmaceuticals, Inc.2015-03-01Not applicableUs
Megestrol AcetateTablet40 mg/1OralNcs Health Care Of Ky, Inc Dba Vangard Labs1988-08-08Not applicableUs
Megestrol AcetateSuspension40 mg/mLOralCardinal Health2014-06-23Not applicableUs
Megestrol AcetateSuspension800 mg/20mLOralPrecision Dose Inc.2007-01-092016-03-17Us
Megestrol AcetateTablet40 mg/1OralCardinal Health2004-02-16Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
MagestinNot Available
MaygaceNot Available
MegeronNot Available
MegestatNot Available
MegestilNot Available
MegestinNot Available
NiagestinNot Available
OvabanNot Available
OvaridNot Available
VolidanNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIITJ2M0FR8ES
CAS number595-33-5
WeightAverage: 370.4819
Monoisotopic: 370.214409448
Chemical FormulaC23H30O4
InChI KeyURXWVWVPMJSAJD-KOORYGTMSA-N
InChI
InChI=1S/C23H30O4/c1-14(24)23(27-15(2)25)12-9-20-18-6-5-16-13-17(26)7-10-21(16,3)19(18)8-11-22(20,23)4/h5-6,13,18-20H,7-12H2,1-4H3/t18-,19+,20+,21+,22+,23+/m1/s1
IUPAC Name
(1S,2R,10R,11S,14R,15S)-14-acetyl-2,15-dimethyl-5-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-6,8-dien-14-yl acetate
SMILES
[H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C=CC2=CC(=O)CC[C@]12C
Pharmacology
IndicationFor the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Also used for the palliative management of recurrent, inoperable, or metastatic breast cancer, endometrial cancer, and prostate cancer in Canada and some other countries.
Structured Indications
PharmacodynamicsMegestrol is a synthetic progestin and has the same physiologic effects as natural progesterone. These effects include induction of secretory changes in the endometrium, increase in basal body temperature, pituitary inhibition, and production of withdrawal bleeding in the presence of estrogen. Mestrogel has slight glucocorticoid activity and very slight mineralocorticoid activity. This drug has no estrogenic, androgenic, or anabolic activity. The precise mechanism of megestrol’s antianorexic and anticachetic effects is unknown. Initially developed as a contraceptive, it was first evaluated in breast cancer treatment in 1967.
Mechanism of actionThe precise mechanism by which megestrol acetate produces effects in anorexia and cachexia is unknown at the present time, but its progestin antitumour activity may involve suppression of luteinizing hormone by inhibition of pituitary function. Studies also suggest that the megestrol's weight gain effect is related to its appetite-stimulant or metabolic effects rather than its glucocorticoid-like effects or the production of edema. It has also been suggested that megestrol may alter metabolic pathyways via interferences with the production or action of mediators such as cachectin, a hormone that inhibits adipocyte lipogenic enzymes.
TargetKindPharmacological actionActionsOrganismUniProt ID
Progesterone receptorProteinyes
agonist
HumanP06401 details
Glucocorticoid receptorProteinunknown
agonist
HumanP04150 details
Related Articles
AbsorptionVariable, but well absorbed orally.
Volume of distributionNot Available
Protein bindingNot Available
Metabolism

Primarily hepatic. Megestrol metabolites which were identified in urine constituted 5% to 8% of the dose administered. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces. No active metabolites have been identified.

Route of eliminationThe major route of drug elimination in humans is urine. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces.
Half life34 hours
ClearanceNot Available
ToxicityNo serious unexpected side effects have resulted from studies involving megestrol acetate oral suspension administered in dosages as high as 1200 mg/day. Treatment with megestrol acetate, an orexigenic agent, has also resulted in iatrogenic adrenal suppression. The mechanism is presumably related to the glucocorticoid properties of megestrol acetate [PMID: 12872362].
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Megestrol acetate.Approved
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Megestrol acetate.Approved, Investigational
AcebutololThe serum concentration of Acebutolol can be increased when it is combined with Megestrol acetate.Approved
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Megestrol acetate.Approved
AcetaminophenThe serum concentration of Acetaminophen can be increased when it is combined with Megestrol acetate.Approved
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Megestrol acetate.Withdrawn
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Megestrol acetate.Approved
Acetylsalicylic acidThe serum concentration of Acetylsalicylic acid can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
AfatinibThe serum concentration of Afatinib can be increased when it is combined with Megestrol acetate.Approved
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Megestrol acetate.Experimental
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Megestrol acetate.Experimental
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Megestrol acetate.Approved, Investigational
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Megestrol acetate.Approved
AmbrisentanThe serum concentration of Ambrisentan can be increased when it is combined with Megestrol acetate.Approved, Investigational
AmitriptylineThe serum concentration of Amitriptyline can be increased when it is combined with Megestrol acetate.Approved
AncrodThe therapeutic efficacy of Ancrod can be decreased when used in combination with Megestrol acetate.Investigational
Antithrombin III humanThe therapeutic efficacy of Antithrombin III human can be decreased when used in combination with Megestrol acetate.Approved
AnvirzelAnvirzel may decrease the cardiotoxic activities of Megestrol acetate.Investigational
ApixabanThe therapeutic efficacy of Apixaban can be decreased when used in combination with Megestrol acetate.Approved
ArdeparinThe therapeutic efficacy of Ardeparin can be decreased when used in combination with Megestrol acetate.Approved, Withdrawn
ArgatrobanThe therapeutic efficacy of Argatroban can be decreased when used in combination with Megestrol acetate.Approved, Investigational
Arsenic trioxideThe serum concentration of Arsenic trioxide can be increased when it is combined with Megestrol acetate.Approved, Investigational
AtazanavirThe serum concentration of Atazanavir can be increased when it is combined with Megestrol acetate.Approved, Investigational
AtenololThe serum concentration of Atenolol can be increased when it is combined with Megestrol acetate.Approved
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Megestrol acetate.Approved, Investigational
BalaglitazoneThe therapeutic efficacy of Balaglitazone can be decreased when used in combination with Megestrol acetate.Investigational
BecaplerminThe therapeutic efficacy of Becaplermin can be decreased when used in combination with Megestrol acetate.Approved, Investigational
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Megestrol acetate.Approved, Investigational
BivalirudinThe therapeutic efficacy of Bivalirudin can be decreased when used in combination with Megestrol acetate.Approved, Investigational
BoceprevirThe serum concentration of Boceprevir can be increased when it is combined with Megestrol acetate.Approved
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Megestrol acetate.Approved
Brentuximab vedotinThe serum concentration of Brentuximab vedotin can be increased when it is combined with Megestrol acetate.Approved
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Megestrol acetate.Approved, Investigational
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Megestrol acetate.Withdrawn
C1 Esterase Inhibitor (Human)Megestrol acetate may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).Approved
C1 Esterase Inhibitor (Recombinant)Megestrol acetate may increase the thrombogenic activities of C1 Esterase Inhibitor (Recombinant).Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Megestrol acetate.Approved
CaffeineThe serum concentration of Caffeine can be increased when it is combined with Megestrol acetate.Approved
CamptothecinThe serum concentration of Camptothecin can be increased when it is combined with Megestrol acetate.Experimental
CanagliflozinThe serum concentration of Canagliflozin can be increased when it is combined with Megestrol acetate.Approved
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Megestrol acetate.Approved, Investigational
CarfilzomibThe serum concentration of Carfilzomib can be increased when it is combined with Megestrol acetate.Approved
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Megestrol acetate.Experimental
CeritinibThe serum concentration of Ceritinib can be increased when it is combined with Megestrol acetate.Approved
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Megestrol acetate.Withdrawn
CertoparinThe therapeutic efficacy of Certoparin can be decreased when used in combination with Megestrol acetate.Approved
ChlorpromazineThe serum concentration of Chlorpromazine can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Megestrol acetate.Approved
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Megestrol acetate.Experimental
CimetidineThe serum concentration of Cimetidine can be increased when it is combined with Megestrol acetate.Approved
CiprofloxacinThe serum concentration of Ciprofloxacin can be increased when it is combined with Megestrol acetate.Approved, Investigational
CisplatinThe serum concentration of Cisplatin can be increased when it is combined with Megestrol acetate.Approved
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Megestrol acetate.Approved
Citric AcidThe therapeutic efficacy of Citric Acid can be decreased when used in combination with Megestrol acetate.Nutraceutical, Vet Approved
ClarithromycinThe serum concentration of Clarithromycin can be increased when it is combined with Megestrol acetate.Approved
ClobazamThe serum concentration of Clobazam can be increased when it is combined with Megestrol acetate.Approved, Illicit
ClomifeneThe serum concentration of Clomifene can be increased when it is combined with Megestrol acetate.Approved, Investigational
ClonidineThe serum concentration of Clonidine can be increased when it is combined with Megestrol acetate.Approved
ClopidogrelThe serum concentration of Clopidogrel can be increased when it is combined with Megestrol acetate.Approved, Nutraceutical
ClozapineThe serum concentration of Clozapine can be increased when it is combined with Megestrol acetate.Approved
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Megestrol acetate.Approved
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Megestrol acetate.Approved
Conjugated Equine EstrogensThe serum concentration of Conjugated Equine Estrogens can be increased when it is combined with Megestrol acetate.Approved
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Megestrol acetate.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Megestrol acetate.Approved, Investigational
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
Dabigatran etexilateThe serum concentration of the active metabolites of Dabigatran etexilate can be increased when Dabigatran etexilate is used in combination with Megestrol acetate.Approved
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Megestrol acetate.Approved
DactinomycinThe serum concentration of Dactinomycin can be increased when it is combined with Megestrol acetate.Approved
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Megestrol acetate.Approved
DanaparoidThe therapeutic efficacy of Danaparoid can be decreased when used in combination with Megestrol acetate.Approved, Withdrawn
DapagliflozinThe serum concentration of Dapagliflozin can be increased when it is combined with Megestrol acetate.Approved
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Megestrol acetate.Approved, Investigational
DaunorubicinThe serum concentration of Daunorubicin can be increased when it is combined with Megestrol acetate.Approved
DebrisoquinThe serum concentration of Debrisoquin can be increased when it is combined with Megestrol acetate.Approved
DeoxyspergualinThe therapeutic efficacy of Deoxyspergualin can be decreased when used in combination with Megestrol acetate.Investigational
DesirudinThe therapeutic efficacy of Desirudin can be decreased when used in combination with Megestrol acetate.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Megestrol acetate.Approved
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
DextranThe therapeutic efficacy of Dextran can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
Dextran 40The therapeutic efficacy of Dextran 40 can be decreased when used in combination with Megestrol acetate.Approved
Dextran 70The therapeutic efficacy of Dextran 70 can be decreased when used in combination with Megestrol acetate.Approved
Dextran 75The therapeutic efficacy of Dextran 75 can be decreased when used in combination with Megestrol acetate.Approved
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Megestrol acetate.Approved, Illicit, Vet Approved
DicoumarolThe therapeutic efficacy of Dicoumarol can be decreased when used in combination with Megestrol acetate.Approved
DiethylstilbestrolThe serum concentration of Diethylstilbestrol can be increased when it is combined with Megestrol acetate.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Megestrol acetate.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Megestrol acetate.Approved
DihydrotestosteroneThe serum concentration of Dihydrotestosterone can be increased when it is combined with Megestrol acetate.Illicit
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Megestrol acetate.Approved
DipyridamoleThe serum concentration of Dipyridamole can be increased when it is combined with Megestrol acetate.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Megestrol acetate.Approved, Investigational
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Megestrol acetate.Approved
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Megestrol acetate.Approved, Investigational
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Megestrol acetate.Approved
Edetic AcidThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Megestrol acetate.Approved, Vet Approved
EdoxabanThe serum concentration of Edoxaban can be increased when it is combined with Megestrol acetate.Approved
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Megestrol acetate.Approved, Investigational
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Megestrol acetate.Approved
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Megestrol acetate.Approved
EpinastineThe serum concentration of Epinastine can be increased when it is combined with Megestrol acetate.Approved, Investigational
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Megestrol acetate.Approved, Investigational
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
EstradiolThe serum concentration of Estradiol can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
EstriolThe serum concentration of Estriol can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
EstroneThe serum concentration of Estrone can be increased when it is combined with Megestrol acetate.Approved
Ethinyl EstradiolThe serum concentration of Ethinyl Estradiol can be increased when it is combined with Megestrol acetate.Approved
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Megestrol acetate.Withdrawn
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Megestrol acetate.Approved
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Megestrol acetate.Approved
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
EzetimibeThe serum concentration of Ezetimibe can be increased when it is combined with Megestrol acetate.Approved
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Megestrol acetate.Approved
FexofenadineThe serum concentration of Fexofenadine can be increased when it is combined with Megestrol acetate.Approved
FidaxomicinThe serum concentration of Fidaxomicin can be increased when it is combined with Megestrol acetate.Approved
FluindioneThe therapeutic efficacy of Fluindione can be decreased when used in combination with Megestrol acetate.Investigational
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Megestrol acetate.Approved
FondaparinuxThe therapeutic efficacy of Fondaparinux can be decreased when used in combination with Megestrol acetate.Investigational
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Megestrol acetate.Approved, Investigational
GabexateThe therapeutic efficacy of Gabexate can be decreased when used in combination with Megestrol acetate.Investigational
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Megestrol acetate.Approved, Investigational
GemcitabineThe serum concentration of Gemcitabine can be increased when it is combined with Megestrol acetate.Approved
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Megestrol acetate.Withdrawn
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Megestrol acetate.Approved
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Megestrol acetate.Approved
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Megestrol acetate.Approved
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Megestrol acetate.Approved
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Megestrol acetate.Approved
GrazoprevirThe serum concentration of Grazoprevir can be increased when it is combined with Megestrol acetate.Approved
GrepafloxacinThe serum concentration of Grepafloxacin can be increased when it is combined with Megestrol acetate.Withdrawn
GusperimusThe therapeutic efficacy of Gusperimus can be decreased when used in combination with Megestrol acetate.Investigational
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Megestrol acetate.Approved
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Megestrol acetate.Approved, Investigational
HirulogThe therapeutic efficacy of Hirulog can be decreased when used in combination with Megestrol acetate.Experimental
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
IbuprofenThe serum concentration of Ibuprofen can be increased when it is combined with Megestrol acetate.Approved
IdelalisibThe serum concentration of Idelalisib can be increased when it is combined with Megestrol acetate.Approved
idraparinuxThe therapeutic efficacy of idraparinux can be decreased when used in combination with Megestrol acetate.Investigational
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Megestrol acetate.Approved
ImipramineThe serum concentration of Imipramine can be increased when it is combined with Megestrol acetate.Approved
IndacaterolThe serum concentration of Indacaterol can be increased when it is combined with Megestrol acetate.Approved
IndinavirThe serum concentration of Indinavir can be increased when it is combined with Megestrol acetate.Approved
IndomethacinThe serum concentration of Indomethacin can be increased when it is combined with Megestrol acetate.Approved, Investigational
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Megestrol acetate.Approved
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Megestrol acetate.Approved
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Megestrol acetate.Approved
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Megestrol acetate.Approved
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Megestrol acetate.Approved
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Megestrol acetate.Approved
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Megestrol acetate.Approved, Investigational
IvermectinThe serum concentration of Ivermectin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
KetazolamThe serum concentration of Ketazolam can be increased when it is combined with Megestrol acetate.Approved
KetoconazoleThe serum concentration of Ketoconazole can be increased when it is combined with Megestrol acetate.Approved, Investigational
LamivudineThe serum concentration of Lamivudine can be increased when it is combined with Megestrol acetate.Approved, Investigational
LamotrigineThe serum concentration of Lamotrigine can be increased when it is combined with Megestrol acetate.Approved, Investigational
LansoprazoleThe serum concentration of Lansoprazole can be increased when it is combined with Megestrol acetate.Approved, Investigational
LedipasvirThe serum concentration of Ledipasvir can be increased when it is combined with Megestrol acetate.Approved
LenalidomideThe serum concentration of Lenalidomide can be increased when it is combined with Megestrol acetate.Approved
LenvatinibThe serum concentration of Lenvatinib can be increased when it is combined with Megestrol acetate.Approved
LepirudinThe therapeutic efficacy of Lepirudin can be decreased when used in combination with Megestrol acetate.Approved
LevetiracetamThe serum concentration of Levetiracetam can be increased when it is combined with Megestrol acetate.Approved, Investigational
LevofloxacinThe serum concentration of Levofloxacin can be increased when it is combined with Megestrol acetate.Approved, Investigational
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Megestrol acetate.Approved
LinagliptinThe serum concentration of Linagliptin can be increased when it is combined with Megestrol acetate.Approved
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Megestrol acetate.Approved
LoperamideThe serum concentration of Loperamide can be increased when it is combined with Megestrol acetate.Approved
LosartanThe serum concentration of Losartan can be increased when it is combined with Megestrol acetate.Approved
MannitolThe serum concentration of Mannitol can be increased when it is combined with Megestrol acetate.Approved, Investigational
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Megestrol acetate.Approved
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Megestrol acetate.Approved
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Megestrol acetate.Approved, Investigational
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Megestrol acetate.Approved, Illicit
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Megestrol acetate.Approved
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Megestrol acetate.Approved
MirabegronThe serum concentration of Mirabegron can be increased when it is combined with Megestrol acetate.Approved
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
MitoxantroneThe serum concentration of Mitoxantrone can be increased when it is combined with Megestrol acetate.Approved, Investigational
MorphineThe serum concentration of Morphine can be increased when it is combined with Megestrol acetate.Approved, Investigational
Mycophenolate mofetilThe serum concentration of Mycophenolate mofetil can be increased when it is combined with Megestrol acetate.Approved, Investigational
NadololThe serum concentration of Nadolol can be increased when it is combined with Megestrol acetate.Approved
NadroparinThe therapeutic efficacy of Nadroparin can be decreased when used in combination with Megestrol acetate.Approved
NafamostatThe therapeutic efficacy of Nafamostat can be decreased when used in combination with Megestrol acetate.Investigational
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Megestrol acetate.Approved
NaloxoneThe serum concentration of Naloxone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
NelfinavirThe serum concentration of Nelfinavir can be increased when it is combined with Megestrol acetate.Approved
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Megestrol acetate.Approved
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Megestrol acetate.Approved
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Megestrol acetate.Approved, Investigational
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Megestrol acetate.Approved
NizatidineThe serum concentration of Nizatidine can be increased when it is combined with Megestrol acetate.Approved
OlanzapineThe serum concentration of Olanzapine can be increased when it is combined with Megestrol acetate.Approved, Investigational
OmbitasvirThe serum concentration of Ombitasvir can be increased when it is combined with Megestrol acetate.Approved
OsimertinibThe serum concentration of Osimertinib can be increased when it is combined with Megestrol acetate.Approved
OtamixabanThe therapeutic efficacy of Otamixaban can be decreased when used in combination with Megestrol acetate.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Megestrol acetate.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Megestrol acetate.Approved, Vet Approved
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Megestrol acetate.Approved, Investigational
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Megestrol acetate.Approved
Pentosan PolysulfateThe therapeutic efficacy of Pentosan Polysulfate can be decreased when used in combination with Megestrol acetate.Approved
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Megestrol acetate.Approved, Withdrawn
PhenindioneThe therapeutic efficacy of Phenindione can be decreased when used in combination with Megestrol acetate.Approved
PhenobarbitalThe serum concentration of Phenobarbital can be increased when it is combined with Megestrol acetate.Approved
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Megestrol acetate.Approved
PhenytoinThe serum concentration of Phenytoin can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Megestrol acetate.Approved, Investigational
PitavastatinThe serum concentration of Pitavastatin can be increased when it is combined with Megestrol acetate.Approved
PomalidomideThe serum concentration of Pomalidomide can be increased when it is combined with Megestrol acetate.Approved
PonatinibThe serum concentration of Ponatinib can be increased when it is combined with Megestrol acetate.Approved
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
PravastatinThe serum concentration of Pravastatin can be increased when it is combined with Megestrol acetate.Approved
PrazosinThe serum concentration of Prazosin can be increased when it is combined with Megestrol acetate.Approved
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
ProgesteroneThe serum concentration of Progesterone can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
PropranololThe serum concentration of Propranolol can be increased when it is combined with Megestrol acetate.Approved, Investigational
Protein CThe therapeutic efficacy of Protein C can be decreased when used in combination with Megestrol acetate.Approved
Protein S humanThe therapeutic efficacy of Protein S human can be decreased when used in combination with Megestrol acetate.Approved
ProtocatechualdehydeThe therapeutic efficacy of Protocatechualdehyde can be decreased when used in combination with Megestrol acetate.Approved
PrucaloprideThe serum concentration of Prucalopride can be increased when it is combined with Megestrol acetate.Approved
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Megestrol acetate.Approved
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Megestrol acetate.Approved
QuinineThe serum concentration of Quinine can be increased when it is combined with Megestrol acetate.Approved
RanitidineThe serum concentration of Ranitidine can be increased when it is combined with Megestrol acetate.Approved
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Megestrol acetate.Approved, Investigational
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
ReserpineThe serum concentration of Reserpine can be increased when it is combined with Megestrol acetate.Approved
ReviparinThe therapeutic efficacy of Reviparin can be decreased when used in combination with Megestrol acetate.Approved
RifampicinThe serum concentration of Rifampicin can be increased when it is combined with Megestrol acetate.Approved
RifaximinThe serum concentration of Rifaximin can be increased when it is combined with Megestrol acetate.Approved, Investigational
RisperidoneThe serum concentration of Risperidone can be increased when it is combined with Megestrol acetate.Approved, Investigational
RitonavirThe serum concentration of Ritonavir can be increased when it is combined with Megestrol acetate.Approved, Investigational
RivaroxabanThe therapeutic efficacy of Rivaroxaban can be decreased when used in combination with Megestrol acetate.Approved
RomidepsinThe serum concentration of Romidepsin can be increased when it is combined with Megestrol acetate.Approved, Investigational
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Megestrol acetate.Approved, Investigational
Salicylic acidThe serum concentration of Salicylic acid can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
SaquinavirThe serum concentration of Saquinavir can be increased when it is combined with Megestrol acetate.Approved, Investigational
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Megestrol acetate.Approved
SelexipagThe serum concentration of Selexipag can be increased when it is combined with Megestrol acetate.Approved
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Megestrol acetate.Approved
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Megestrol acetate.Approved
SitagliptinThe serum concentration of Sitagliptin can be increased when it is combined with Megestrol acetate.Approved, Investigational
SofosbuvirThe serum concentration of Sofosbuvir can be increased when it is combined with Megestrol acetate.Approved
SorafenibThe serum concentration of Sorafenib can be increased when it is combined with Megestrol acetate.Approved, Investigational
SparfloxacinThe serum concentration of Sparfloxacin can be increased when it is combined with Megestrol acetate.Approved
SphingosineThe serum concentration of Sphingosine can be increased when it is combined with Megestrol acetate.Experimental
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Megestrol acetate.Approved, Investigational
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Megestrol acetate.Approved, Investigational
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Megestrol acetate.Approved
Taurocholic AcidThe serum concentration of Taurocholic Acid can be increased when it is combined with Megestrol acetate.Experimental
Technetium Tc-99m sestamibiThe serum concentration of Technetium Tc-99m sestamibi can be increased when it is combined with Megestrol acetate.Approved
TelaprevirThe serum concentration of Telaprevir can be increased when it is combined with Megestrol acetate.Approved
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Megestrol acetate.Approved
ThiazolidinedioneThe therapeutic efficacy of Thiazolidinedione can be decreased when used in combination with Megestrol acetate.Investigational
TicagrelorThe serum concentration of Ticagrelor can be increased when it is combined with Megestrol acetate.Approved
TimololThe serum concentration of Timolol can be increased when it is combined with Megestrol acetate.Approved
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Megestrol acetate.Approved
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Megestrol acetate.Approved
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Megestrol acetate.Approved
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Megestrol acetate.Approved, Investigational
ToremifeneThe serum concentration of Toremifene can be increased when it is combined with Megestrol acetate.Approved, Investigational
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Megestrol acetate.Approved, Investigational
Trastuzumab emtansineThe serum concentration of Trastuzumab emtansine can be increased when it is combined with Megestrol acetate.Approved
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Megestrol acetate.Withdrawn
UlipristalThe therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Ulipristal.Approved
UmeclidiniumThe serum concentration of Umeclidinium can be increased when it is combined with Megestrol acetate.Approved
VecuroniumThe serum concentration of Vecuronium can be increased when it is combined with Megestrol acetate.Approved
VenetoclaxThe serum concentration of Venetoclax can be increased when it is combined with Megestrol acetate.Approved
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Megestrol acetate.Approved
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Megestrol acetate.Approved
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Megestrol acetate.Approved, Investigational
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Megestrol acetate.Approved
VincristineThe serum concentration of Vincristine can be increased when it is combined with Megestrol acetate.Approved, Investigational
VismodegibThe serum concentration of Vismodegib can be increased when it is combined with Megestrol acetate.Approved
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Megestrol acetate.Approved, Investigational
WarfarinThe therapeutic efficacy of Warfarin can be decreased when used in combination with Megestrol acetate.Approved
XimelagatranThe therapeutic efficacy of Ximelagatran can be decreased when used in combination with Megestrol acetate.Approved, Investigational, Withdrawn
Ym150The therapeutic efficacy of Ym150 can be decreased when used in combination with Megestrol acetate.Investigational
ZidovudineThe serum concentration of Zidovudine can be increased when it is combined with Megestrol acetate.Approved
Food Interactions
  • Take with food.
References
Synthesis Reference

Klaus ANNEN, Thomas Linz, Karl-Heinz Neff, Rolf Bohlmann, Henry Laurent, “PROCESS FOR PREPARING 17ALPHA-ACETOXY-6-METHYLENEPREGN-4-ENE-3,20-DIONE, MEDROXYPROGESTERONE ACETATE AND MEGESTROL ACETATE.” U.S. Patent US20090012321, issued January 08, 2009.

US20090012321
General References
  1. Berenstein EG, Ortiz Z: Megestrol acetate for the treatment of anorexia-cachexia syndrome. Cochrane Database Syst Rev. 2005 Apr 18;(2):CD004310. [PubMed:15846706 ]
  2. Pascual Lopez A, Roque i Figuls M, Urrutia Cuchi G, Berenstein EG, Almenar Pasies B, Balcells Alegre M, Herdman M: Systematic review of megestrol acetate in the treatment of anorexia-cachexia syndrome. J Pain Symptom Manage. 2004 Apr;27(4):360-9. [PubMed:15050664 ]
  3. Rao GG, Miller DS: Hormonal therapy in epithelial ovarian cancer. Expert Rev Anticancer Ther. 2006 Jan;6(1):43-7. [PubMed:16375643 ]
  4. Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH: Classification and pharmacology of progestins. Maturitas. 2008 Sep-Oct;61(1-2):171-80. [PubMed:19434889 ]
  5. Orme LM, Bond JD, Humphrey MS, Zacharin MR, Downie PA, Jamsen KM, Mitchell SL, Robinson JM, Grapsas NA, Ashley DM: Megestrol acetate in pediatric oncology patients may lead to severe, symptomatic adrenal suppression. Cancer. 2003 Jul 15;98(2):397-405. [PubMed:12872362 ]
External Links
ATC CodesG03AA04G03DB02L02AB01G03AC05G03FA08G03AB01G03FB04
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (278 KB)
MSDSDownload (71.9 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9959
Blood Brain Barrier+0.9617
Caco-2 permeable+0.651
P-glycoprotein substrateSubstrate0.6107
P-glycoprotein inhibitor IInhibitor0.9149
P-glycoprotein inhibitor IIInhibitor0.7016
Renal organic cation transporterNon-inhibitor0.7753
CYP450 2C9 substrateNon-substrate0.8642
CYP450 2D6 substrateNon-substrate0.908
CYP450 3A4 substrateSubstrate0.7744
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.8907
CYP450 2D6 inhibitorNon-inhibitor0.9532
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8095
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.899
Ames testNon AMES toxic0.9775
CarcinogenicityNon-carcinogens0.9273
BiodegradationNot ready biodegradable0.9354
Rat acute toxicity1.8121 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9429
hERG inhibition (predictor II)Non-inhibitor0.7761
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Bristol myers squibb
  • Par pharmaceutical inc
  • Apotex inc richmond hill
  • Roxane laboratories inc
  • Teva pharmaceuticals usa
  • Wockhardt eu operations (swiss) ag
  • Barr laboratories inc
  • Teva pharmaceuticals usa inc
  • Usl pharma inc
Packagers
Dosage forms
FormRouteStrength
SuspensionOral125 mg/mL
SuspensionOral40 mg
TabletOral160 mg
TabletOral40 mg
SuspensionOral40 mg/mL
SuspensionOral400 mg/10mL
SuspensionOral800 mg/20mL
TabletOral20 mg/1
TabletOral40 mg/1
Prices
Unit descriptionCostUnit
Megestrol Acetate 40 mg/ml Suspension 480ml Bottle297.92USD bottle
Megestrol Acetate 40 mg/ml Suspension 240ml Bottle149.71USD bottle
Megestrol acetate powder30.6USD g
Megestrol 40 mg tablet1.17USD tablet
Megestrol Acetate 40 mg tablet1.15USD tablet
Megestrol Acetate 20 mg tablet0.72USD tablet
Megace 40 mg/ml oral suspension0.71USD ml
Megestrol 20 mg tablet0.65USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5145684 No1994-01-252011-01-25Us
US6592903 No2000-09-212020-09-21Us
US7101576 No2004-04-222024-04-22Us
US9040088 No2004-04-222024-04-22Us
US9101540 No2004-04-222024-04-22Us
US9101549 No2004-04-222024-04-22Us
US9107827 No2004-04-222024-04-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point218.0-220.0 °CNot Available
water solubility2 µg/mL (at 37 °C for the acetate salt)Not Available
logP3.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00338 mg/mLALOGPS
logP2.99ALOGPS
logP3.48ChemAxon
logS-5ALOGPS
pKa (Strongest Acidic)17.83ChemAxon
pKa (Strongest Basic)-4.8ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area60.44 Å2ChemAxon
Rotatable Bond Count3ChemAxon
Refractivity104.37 m3·mol-1ChemAxon
Polarizability41.33 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as gluco/mineralocorticoids, progestogins and derivatives. These are steroids with a structure based on a hydroxylated prostane moiety.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassPregnane steroids
Direct ParentGluco/mineralocorticoids, progestogins and derivatives
Alternative Parents
Substituents
  • Progestogin-skeleton
  • Steroid ester
  • 20-oxosteroid
  • Oxosteroid
  • 3-oxosteroid
  • Alpha-acyloxy ketone
  • Acetate salt
  • Cyclic ketone
  • Ketone
  • Carboxylic acid ester
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Carbonyl group
  • Aliphatic homopolycyclic compound
Molecular FrameworkAliphatic homopolycyclic compounds
External Descriptors

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.Isoform A: inactive in stimulating c-Src/MAPK signaling on hormone stimulation.Isoform 4: Increases mitochondrial ...
Gene Name:
PGR
Uniprot ID:
P06401
Molecular Weight:
98979.96 Da
References
  1. Vadivelu S, Sharer L, Schulder M: Regression of multiple intracranial meningiomas after cessation of long-term progesterone agonist therapy. J Neurosurg. 2010 May;112(5):920-4. doi: 10.3171/2009.8.JNS09201. [PubMed:19731987 ]
  2. Mokbel K: Focus on anastrozole and breast cancer. Curr Med Res Opin. 2003;19(8):683-8. [PubMed:14687437 ]
  3. Wentling GK, Sevin BU, Geiger XJ, Bridges MD: Benign metastasizing leiomyoma responsive to megestrol: case report and review of the literature. Int J Gynecol Cancer. 2005 Nov-Dec;15(6):1213-7. [PubMed:16343217 ]
  4. Gruber T, Dare AO, Balos LL, Lele S, Fenstermaker RA: Multiple meningiomas arising during long-term therapy with the progesterone agonist megestrol acetate. Case report. J Neurosurg. 2004 Feb;100(2):328-31. [PubMed:15086241 ]
  5. Schindler AE, Campagnoli C, Druckmann R, Huber J, Pasqualini JR, Schweppe KW, Thijssen JH: Classification and pharmacology of progestins. Maturitas. 2008 Sep-Oct;61(1-2):171-80. [PubMed:19434889 ]
  6. Wermers RA, Hurley DL, Kearns AE: Osteoporosis associated with megestrol acetate. Mayo Clin Proc. 2004 Dec;79(12):1557-61. [PubMed:15595341 ]
  7. Wiedemann K, Hirschmann M, Knaudt K, Rupprecht R, Seier FE, Holsboer F: Sleep endocrine effects of megestrol acetate in healthy men. J Neuroendocrinol. 1998 Sep;10(9):719-27. [PubMed:9744490 ]
  8. Lamberts SW, Uitterlinden P, Bons EG, Verleun T: Comparison of the actions of RU 38486 and megestrol acetate in the model of a transplantable adrenocorticotropin- and prolactin-secreting rat pituitary tumor. Cancer Res. 1985 Mar;45(3):1015-9. [PubMed:2982481 ]
  9. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Receptor for glucocorticoids (GC). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors. Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Could act as a coactivator for STAT5-dependent transcription upon grow...
Gene Name:
NR3C1
Uniprot ID:
P04150
Molecular Weight:
85658.57 Da
References
  1. Wermers RA, Hurley DL, Kearns AE: Osteoporosis associated with megestrol acetate. Mayo Clin Proc. 2004 Dec;79(12):1557-61. [PubMed:15595341 ]
  2. Gonzalez Villarroel P, Fernandez Perez I, Paramo C, Gentil Gonzalez M, Carnero Lopez B, Vazquez Tunas ML, Carrasco Alvarez JA: Megestrol acetate-induced adrenal insufficiency. Clin Transl Oncol. 2008 Apr;10(4):235-7. [PubMed:18411198 ]
  3. Wiedemann K, Hirschmann M, Knaudt K, Rupprecht R, Seier FE, Holsboer F: Sleep endocrine effects of megestrol acetate in healthy men. J Neuroendocrinol. 1998 Sep;10(9):719-27. [PubMed:9744490 ]
  4. Chao Y, Chan WK, Wang SS, Lai KH, Chi CW, Lin CY, Chan A, Whang-Peng J, Lui WY, Lee SD: Phase II study of megestrol acetate in the treatment of hepatocellular carcinoma. J Gastroenterol Hepatol. 1997 Apr;12(4):277-81. [PubMed:9195366 ]
  5. Lamberts SW, Uitterlinden P, Bons EG, Verleun T: Comparison of the actions of RU 38486 and megestrol acetate in the model of a transplantable adrenocorticotropin- and prolactin-secreting rat pituitary tumor. Cancer Res. 1985 Mar;45(3):1015-9. [PubMed:2982481 ]
  6. Kontula K, Paavonen T, Luukkainen T, Andersson LC: Binding of progestins to the glucocorticoid receptor. Correlation to their glucocorticoid-like effects on in vitro functions of human mononuclear leukocytes. Biochem Pharmacol. 1983 May 1;32(9):1511-8. [PubMed:6222739 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Wang L, Yang CP, Horwitz SB, Trail PA, Casazza AM: Reversal of the human and murine multidrug-resistance phenotype with megestrol acetate. Cancer Chemother Pharmacol. 1994;34(2):96-102. [PubMed:8194172 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on December 03, 2016 02:45