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Identification
NameMegestrol acetate
Accession NumberDB00351  (APRD01092)
TypeSmall Molecule
GroupsApproved, Vet Approved
Description

17-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. [PubChem]

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
Magestin
Maygace
Megace
Megeron
Megestat
Megestil
Megestin
MGA
Niagestin
Ovaban
Ovarid
Volidan
External Identifiers Not Available
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.2009-06-012016-04-23Us
Megacetablet40 mgoralBristol Myers Squibb Canada1977-12-312006-05-29Canada
Megace Essuspension125 mg/mLoralPhysicians Total Care, Inc.2006-04-132016-04-05Us
Megace Essuspension125 mg/mLoralPar Pharmaceutical, Inc2005-07-022016-04-05Us
Megace Essuspension125 mg/mLoralAtlantic Biologicals Corps2005-07-022016-04-05Us
Megace Essuspension125 mg/mLoralStat Rx USA2005-06-082016-04-05Us
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.2015-07-282016-04-05Us
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
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-megestroltablet160 mgoralApotex IncNot applicableNot applicableCanada
Apo-megestroltablet40 mgoralApotex IncNot applicableNot applicableCanada
Megestolsuspension40 mg/mLoralSTAT Rx USA LLC2002-02-152016-04-05Us
Megestrol Acetatetablet20 mg/1oralMylan Institutional Inc.1997-08-072016-04-05Us
Megestrol Acetatetablet40 mg/1oralNcs Health Care Of Ky, Inc Dba Vangard Labs1988-08-082016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralRoxane Laboratories, Inc2002-02-152016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralPrecision Dose Inc.2014-06-232016-04-05Us
Megestrol Acetatetablet20 mg/1oralCardinal Health2011-05-132016-04-05Us
Megestrol Acetatetablet40 mg/1oralState of Florida DOH Central Pharmacy2009-07-012016-04-05Us
Megestrol Acetatesuspension40 mg/mLoralPrecision Dose Inc.2014-10-082016-04-05Us
Megestrol Acetatesuspension40 mg/mLoralPar Pharmaceutical, Inc.2001-07-252016-04-05Us
Megestrol Acetatetablet40 mg/1oralBarr Laboratories Inc.1995-11-302016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralVista Pharm, Inc.2012-08-222016-04-05Us
Megestrol Acetatesuspension40 mg/mLoralCardinal Health2014-06-232016-04-05Us
Megestrol Acetatetablet40 mg/1oralPar Pharmaceutical Inc1988-08-082016-04-05Us
Megestrol Acetatetablet20 mg/1oralBarr Laboratories Inc.1996-10-252016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2013-03-082016-04-05Us
Megestrol Acetatesuspension400 mg/10mLoralCardinal Health2004-02-252016-04-05Us
Megestrol Acetatetablet40 mg/1oralMc Kesson Packaging Services A Business Unit Of Mc Kesson Corporation2007-08-202016-04-05Us
Megestrol Acetatesuspension400 mg/10mLoralCardinal Health2004-02-252016-04-05Us
Megestrol Acetatetablet20 mg/1oralPar Pharmaceutical Inc1988-08-082016-04-05Us
Megestrol Acetatesuspension40 mg/mLoralPharmaceutical Associates, Inc.2006-07-072016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralMorton Grove Pharmaceuticals, Inc.2005-02-092016-04-05Us
Megestrol Acetatetablet40 mg/1oralCardinal Health1995-11-302016-04-05Us
Megestrol Acetatetablet40 mg/1oralUDL Laboratories, Inc.2011-05-132015-12-29Us
Megestrol Acetatesuspension125 mg/mLoralT Wi Pharmaceuticals, Inc.2015-03-012016-04-05Us
Megestrol Acetatetablet40 mg/1oralRoxane Laboratories, Inc1995-09-292016-04-23Us
Megestrol Acetatetablet40 mg/1oralGolden State Medical Supply, Inc.2015-09-042016-04-05Us
Megestrol Acetatetablet40 mg/1oralCardinal Health2004-02-162016-04-05Us
Megestrol Acetatetablet40 mg/1oralAvera Mc Kennan Hospital2015-03-022016-04-05Us
Megestrol Acetatesuspension40 mg/mLoralAtlantic Biologicals Corps2001-07-252016-04-05Us
Megestrol Acetatetablet20 mg/1oralRoxane Laboratories, Inc1995-09-292016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralPhysicians Total Care, Inc.2005-09-012016-04-05Us
Megestrol Acetatesuspension400 mg/10mLoralPrecision Dose Inc.2004-02-252016-03-17Us
Megestrol Acetatetablet40 mg/1oralRoxane Laboratories, Inc1995-09-292016-04-23Us
Megestrol Acetatesuspension40 mg/mLoralCardinal Health2006-07-072016-04-05Us
Megestrol Acetatetablet40 mg/1oralMajor Pharmaceuticals2004-02-162016-04-05Us
Megestrol Acetatetablet20 mg/1oralRoxane Laboratories, Inc1995-09-292016-04-23Us
Megestrol Acetatetablet40 mg/1oralCardinal Health2011-05-132016-04-05Us
Megestrol Acetatetablet40 mg/1oralPhysicians Total Care, Inc.2007-07-052016-04-05Us
Megestrol Acetatesuspension800 mg/20mLoralPrecision Dose Inc.2007-01-092016-03-17Us
Over the Counter ProductsNot Available
International Brands
NameCompany
MaygaceNot Available
MegestilNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIITJ2M0FR8ES
CAS number595-33-5
WeightAverage: 370.4819
Monoisotopic: 370.214409448
Chemical FormulaC23H30O4
InChI KeyInChIKey=URXWVWVPMJSAJD-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
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
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.
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.
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
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
Suspensionoral40 mg/mL
Suspensionoral125 mg/mL
Suspensionoral40 mg
Tabletoral160 mg
Tabletoral40 mg
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
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 CodesNot Available
AHFS Codes
  • 10:00.00
PDB EntriesNot Available
FDA labelDownload (278 KB)
MSDSDownload (71.9 KB)
Interactions
Drug Interactions
Drug
AbciximabThe therapeutic efficacy of Abciximab can be decreased when used in combination with Megestrol acetate.
AcenocoumarolThe therapeutic efficacy of Acenocoumarol can be decreased when used in combination with Megestrol acetate.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Megestrol acetate.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Megestrol acetate.
C1 Esterase Inhibitor (Human)Megestrol acetate may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Megestrol acetate.
CapromabMegestrol acetate may decrease effectiveness of Capromab as a diagnostic agent.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Megestrol acetate.
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Megestrol acetate.
Citric AcidThe therapeutic efficacy of Citric Acid can be decreased when used in combination with Megestrol acetate.
DalteparinThe therapeutic efficacy of Dalteparin can be decreased when used in combination with Megestrol acetate.
DicoumarolThe therapeutic efficacy of Dicoumarol can be decreased when used in combination with Megestrol acetate.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Megestrol acetate.
Edetic AcidThe therapeutic efficacy of Edetic Acid can be decreased when used in combination with Megestrol acetate.
EnoxaparinThe therapeutic efficacy of Enoxaparin can be decreased when used in combination with Megestrol acetate.
Ethyl biscoumacetateThe therapeutic efficacy of Ethyl biscoumacetate can be decreased when used in combination with Megestrol acetate.
Fondaparinux sodiumThe therapeutic efficacy of Fondaparinux sodium can be decreased when used in combination with Megestrol acetate.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Megestrol acetate.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Megestrol acetate.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Megestrol acetate.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Megestrol acetate.
HeparinThe therapeutic efficacy of Heparin can be decreased when used in combination with Megestrol acetate.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Megestrol acetate.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Megestrol acetate.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Megestrol acetate.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Megestrol acetate.
Insulin HumanThe therapeutic efficacy of Insulin Regular can be decreased when used in combination with Megestrol acetate.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Megestrol acetate.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Megestrol acetate.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Megestrol acetate.
PhenindioneThe therapeutic efficacy of Phenindione can be decreased when used in combination with Megestrol acetate.
PhenprocoumonThe therapeutic efficacy of Phenprocoumon can be decreased when used in combination with Megestrol acetate.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Megestrol acetate.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Megestrol acetate.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Megestrol acetate.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Megestrol acetate.
TreprostinilThe therapeutic efficacy of Treprostinil can be decreased when used in combination with Megestrol acetate.
UlipristalThe therapeutic efficacy of Megestrol acetate can be decreased when used in combination with Ulipristal.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Megestrol acetate.
WarfarinThe therapeutic efficacy of Warfarin can be decreased when used in combination with Megestrol acetate.
Food Interactions
  • Take with food.

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 ]
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Drug created on June 13, 2005 07:24 / Updated on May 03, 2016 02:29