MEGESTROL

First approved in 1971

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C22H30O3
Molecular Weight	342.4718
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CC[C@](O)(C(C)=O)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])C=C(C)C4=CC(=O)CC[C@]34C

InChI

InChIKey=VXIMPSPISRVBPZ-NWUMPJBXSA-N

InChI=1S/C22H30O3/c1-13-11-16-17(20(3)8-5-15(24)12-19(13)20)6-9-21(4)18(16)7-10-22(21,25)14(2)23/h11-12,16-18,25H,5-10H2,1-4H3/t16-,17+,18+,20-,21+,22+/m1/s1

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/?term=23395103

Megestrol acetate is 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. MEGACE Oral Suspension is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). The 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. The major route of drug elimination in humans is urine. When radiolabeled megestrol acetate was administered to humans in doses of 4 to 90 mg, the urinary excretion within 10 days ranged from 56.5% to 78.4% (mean 66.4%) and fecal excretion ranged from 7.7% to 30.3% (mean 19.8%). The total recovered radioactivity varied between 83.1% and 94.7% (mean 86.2%). Megestrol acetate 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. Plasma steady-state pharmacokinetics of megestrol acetate were evaluated in 10 adult, cachectic male patients with acquired immunodeficiency syndrome (AIDS) and an involuntary weight loss greater than 10% of baseline. Patients received single oral doses of 800 mg/day of MEGACE Oral Suspension for 21 days. Plasma concentration data obtained on day 21 were evaluated for up to 48 hours past the last dose.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Progesterone receptor 61 Target ID: CHEMBL208 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15086241	Agonist 2662

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anorexia 5 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf	Palliative		Approved 8360	MEGACE Approved Use Megestrol acetate oral suspension is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Launch Date 7.4761922E11
Cachexia 8 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf	Palliative		Approved 8360	MEGACE Approved Use Megestrol acetate oral suspension is indicated for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS). Launch Date 7.4761922E11

C_max

Value	Dose	Analyte	Population
753 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
490 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	750 mg 1 times / day steady-state, oral dose: 750 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
1133 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1618 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1364 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
187 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
10476 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
6779 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	750 mg 1 times / day steady-state, oral dose: 750 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: MALE food status: UNKNOWN
12095 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
16268 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
18625 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8942 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
33.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
39.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	625 mg single, oral dose: 625 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
32.84 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
31.38 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/19774117/	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15595341	unhealthy, 54-68 years n = 2 Health Status: unhealthy Age Group: 54-68 years Sex: F Population Size: 2 Sources: https://pubmed.ncbi.nlm.nih.gov/15595341	Disc. AE: Osteoporosis... AEs leading to discontinuation/dose reduction: Osteoporosis (2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/15595341
625 mg 1 times / day multiple, oral Recommended Dose: 625 mg, 1 times / day Route: oral Route: multiple Dose: 625 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27218795	unhealthy, 65 years n = 1 Health Status: unhealthy Age Group: 65 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/27218795	Disc. AE: Adrenal insufficiency... AEs leading to discontinuation/dose reduction: Adrenal insufficiency (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/27218795
40 mg 2 times / day multiple, oral Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	unhealthy, 85 years n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 85 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	Disc. AE: Deep vein thrombosis... AEs leading to discontinuation/dose reduction: Deep vein thrombosis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16563066
400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	unhealthy, 86 years n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 86 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	Disc. AE: Deep vein thrombosis... AEs leading to discontinuation/dose reduction: Deep vein thrombosis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/16563066
1600 mg 1 times / day multiple, oral Highest studied dose Dose: 1600 mg, 1 times / day Route: oral Route: multiple Dose: 1600 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/3368800	unhealthy Health Status: unhealthy Condition: advanced breast cancer Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/3368800	Sources: https://pubmed.ncbi.nlm.nih.gov/3368800

AEs

AE	Significance	Dose	Population
Osteoporosis	2 patients Disc. AE	400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/15595341	unhealthy, 54-68 years n = 2 Health Status: unhealthy Age Group: 54-68 years Sex: F Population Size: 2 Sources: https://pubmed.ncbi.nlm.nih.gov/15595341
Adrenal insufficiency	1 patient Disc. AE	625 mg 1 times / day multiple, oral Recommended Dose: 625 mg, 1 times / day Route: oral Route: multiple Dose: 625 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27218795	unhealthy, 65 years n = 1 Health Status: unhealthy Age Group: 65 years Sex: M Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/27218795
Deep vein thrombosis	1 patient Disc. AE	40 mg 2 times / day multiple, oral Dose: 40 mg, 2 times / day Route: oral Route: multiple Dose: 40 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	unhealthy, 85 years n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 85 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16563066
Deep vein thrombosis	1 patient Disc. AE	400 mg 2 times / day multiple, oral Dose: 400 mg, 2 times / day Route: oral Route: multiple Dose: 400 mg, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/16563066	unhealthy, 86 years n = 1 Health Status: unhealthy Condition: Alzheimer's disease Age Group: 86 years Sex: F Population Size: 1 Sources: https://pubmed.ncbi.nlm.nih.gov/16563066

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1579 inducer 768 substrate 1709	inhibitor 1752 inducer 383 substrate 1010	inhibitor 1837 substrate 1193

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 704 CYP2C19 1463	CYP3A5 391 CYP1A2 1032 CYP2A6 523 CYP2B6 660 CYP2C8 688 CYP2C19 985 CYP2E1 648 CYP4A11 102	CYP1A2 689

Drug as perpetrator

Target	Modality	Activity
CYP2A6 736	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2C19 1537	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP1A2 1673	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP2C9 1803	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP3A4 1909	inducer 1542 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP1A2 1673	activator 210 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP2E1 964	activator 210 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP3A4 1909	inhibitor 3240 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Inhibition 50 uM]

Drug as victim

Target	Modality	Activity
CYP1A2 1032	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2A6 523	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2B6 660	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C19 985	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C8 688	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C9 1010	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2D6 1193	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2E1 648	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP4A11 102	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP3A4 1709	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	yes
CYP3A5 391	substrate 3326 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	yes

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:6722	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:6722
ZINC	ZINC000033902346	http://zinc15.docking.org/substances/ZINC000033902346

PubMed

Title	Date	PubMed
Reversal effects of nomegestrol acetate on multidrug resistance in adriamycin-resistant MCF7 breast cancer cell line.	2001	11434876
A comparison of megestrol acetate, nandrolone decanoate and dietary counselling for HIV associated weight loss.	2001 Aug	11454075
Implant contraception.	2001 Dec	11727176
Inhibitory effect of nomegestrol acetate on steroidogenesis of cultured granulosa cells from rat ovary in vitro.	2001 Jan	11730560
Megestrol treatment in patients with hepatocellular carcinoma.	2001 Nov 16	11720452
Effects of different types of hormone replacement therapy on mammographic density.	2001 Nov 30	11716994
The impact of hormonal treatments on quality of life of patients with metastatic breast cancer.	2002	12117073
Estrogen as therapy for breast cancer.	2002	12100736
Tamoxifen resistant and refractory breast cancer: the value of aromatase inhibitors.	2002	11929341
Fertility-preserving treatment in young patients with endometrial adenocarcinoma.	2002 Apr 15	12001117
Effect of megestrol caproate on the reproductive function of laboratory animals.	2002 Jun	12447469
Approval summary: letrozole in the treatment of postmenopausal women with advanced breast cancer.	2002 Mar	11895893
[Low-grade sarcoma of the endometrial stroma: late recurrence with ureteral and bladder involvement].	2002 Oct	12455286
Discovery of molecular mechanisms of neuroprotection using cell-based bioassays and oligonucleotide arrays.	2002 Oct 29	12388792
Should aromatase inhibitors replace tamoxifen?	2003 Aug	12966738
Acute effects of megestrol on the hypothalamic-pituitary-adrenal axis.	2003 Dec	13680163
[Comparison of changes in biochemical markers of bone turnover after 6 months of hormone replacement therapy with either transdermal 17 beta-estradiol or equine conjugated estrogen plus nomegestrol acetate].	2003 May	14567121
Cancer cachexia.	2003 Nov 5	14613583
Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy.	2004	14680484
Osteoporosis associated with megestrol acetate.	2004 Dec	15595341
Therapy for unresectable hepatocellular carcinoma: review of the randomized clinical trials-II: systemic and local non-embolization-based therapies in unresectable and advanced hepatocellular carcinoma.	2004 Jun	15166617
Cost utility and budget impact of third-generation aromatase inhibitors for advanced breast cancer: a literature-based model analysis of costs in the Italian National Health Service.	2004 Sep	15531017
Clinical utility of serum HER2/neu in monitoring and prediction of progression-free survival in metastatic breast cancer patients treated with trastuzumab-based therapies.	2005	15987448
The science of megestrol acetate delivery: potential to improve outcomes in cachexia.	2005	15984902
Retrospective review of megestrol use for weight loss in an elderly veteran population.	2005 Apr	16548634
Effects of the combined treatment with thalidomide, megestrol and interleukine-2 in cirrhotic patients with advanced hepatocellular carcinoma. A pilot study.	2005 Apr	15788209
Treatment with inhibitors of angiogenesis in advanced hepatocellular carcinoma: a new tool in our hands or simply a hope?	2005 Apr	15788205
[Actions of a 19-norprogesterone derivative on mammary gland: nomegestrol acetate].	2005 Feb	15767920
Effect of nomegestrol acetate on estrogen biosynthesis and transformation in MCF-7 and T47-D breast cancer cells.	2005 Jan	15748827
Control of sulfatase activity by nomegestrol acetate in normal and cancerous human breast tissues.	2005 Jul-Aug	16080533
Nomegestrol acetate may enhance the skeletal effects of estradiol on biochemical markers of bone turnover in menopausal women after a 12-week treatment period.	2005 Jun	16096169
Pregnancy following intracytoplasmic sperm injection and preimplantation genetic diagnosis after the conservative management of endometrial cancer.	2005 Jun	15970008
Antigenotoxic effects of ascorbic acid against megestrol acetate-induced genotoxicity in mice.	2005 Mar	15901051
Hormonal treatment of a recurrent granulosa cell tumor of the ovary: case report and review of the literature.	2005 Mar	15721440
Phase II study of sequential hormonal therapy with anastrozole/exemestane in advanced and metastatic breast cancer.	2005 May 9	15856035
[Isolation and identification of two new epimer from the mother liquid of megestrol acetate].	2005 Sep	16342686
Review of cost-effectiveness analyses in hormonal therapies in advanced breast cancer.	2005 Sep	16144501
Megestrol attenuates the hormonal response to CCK-4-induced panic attacks.	2006	16470820
Hepatocellular carcinoma--Pathological complete response to oral capecitabine, megestrol and thalidomide.	2006	16464803
Effects of a single Silastic contraceptive implant containing nomegestrol acetate (Uniplant) on endometrial morphology and ovarian function for 1 year.	2006 Dec	17157108
Effects of estrogen, raloxifene, and hormone replacement therapy on serum C-reactive protein and homocysteine levels.	2006 Feb 20	15990257
Short-term progestin treatments prevent estrous induction by a GnRH agonist implant in anestrous bitches.	2006 Jan 20	15975646
Orchiectomy or androgen receptor blockade attenuates baroreflex-mediated bradycardia in conscious rats.	2006 Jan 23	16430770
A successful live birth through in vitro fertilization program after conservative treatment of FIGO grade I endometrial cancer.	2006 Jun	16778408
Characterization of related impurities in megestrol acetate.	2006 Jun 16	16616448
Cyclic progestin administration increases energy expenditure and decreases body fat mass in perimenopausal women.	2006 Mar-Apr	16645533
New progestagens for contraceptive use.	2006 Mar-Apr	16291771
Activation of nitric oxide synthesis in human endothelial cells using nomegestrol acetate.	2006 Oct	17012461
Testosterone supplementation of megestrol therapy does not enhance lean tissue accrual in men with human immunodeficiency virus-associated weight loss: a randomized, double-blind, placebo-controlled, multicenter trial.	2007 Feb	17090640
Longitudinal evaluation of serum leptin and bone mineral density in early postmenopausal women.	2007 May-Jun	17242633

Patents

Sample Use Guides

In Vivo Use Guide

Oral Suspension is 800 mg/day (20 mL/day). In clinical trials evaluating different dose schedules, daily doses of 400 and 800 mg/day.

Route of Administration: Oral

In Vitro Use Guide

Megestrol acetate was shown to inhibit the growth of HepG2 cells in vitro in dose- and time-dependent manners with an IC (50) of 260 uM (24-h incubation)

Name

Type

Language

MEGESTROL

Official Name

English

MEGESTROL ACETATE IMPURITY B [EP IMPURITY]

Common Name

English

MEGESTROL [VANDF]

Common Name

English

MEGESTROL [HSDB]

Common Name

English

Megestrol [WHO-DD]

Common Name

English

17-HYDROXY-6-METHYLPREGNA-4,6-DIENE-3,20-DIONE

Systematic Name

English

CHRONOPIL

Brand Name

English

megestrol [INN]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QG03AC05