MEGESTROL ACETATE

First approved in 1971

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H32O4
Molecular Weight	384.5085
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(=O)O[C@@]1(CC[C@H]2[C@@H]3C=C(C)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C)C(C)=O

InChI

InChIKey=RQZAXGRLVPAYTJ-GQFGMJRRSA-N

InChI=1S/C24H32O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h12-13,18-20H,6-11H2,1-5H3/t18-,19+,20+,22-,23+,24+/m1/s1

HIDE SMILES / InChI

Molecular Formula	C24H32O4
Molecular Weight	384.5085
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

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 2752

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anorexia 5 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf	Palliative		Approved 8583	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 1993
Cachexia 9 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf	Palliative		Approved 8583	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 1993

C_max

Value	Dose	Analyte	Population
1364 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	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: UNKNOWN food status: FED
1616 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	675 mg single, oral dose: 675 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
187 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	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: UNKNOWN food status: FASTED
1044 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	675 mg single, oral dose: 675 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN 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
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
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
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

AUC

Value	Dose	Analyte	Population
18625 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	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: UNKNOWN food status: FED
17029 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	675 mg single, oral dose: 675 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
8942 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	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: UNKNOWN food status: FASTED
11879 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2007/021778s002s003lbl.pdf	675 mg single, oral dose: 675 mg route of administration: Oral experiment type: SINGLE co-administered:	MEGESTROL ACETATE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN 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
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
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
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 Health Status: unhealthy Age Group: 54-68 years Sex: F 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 Health Status: unhealthy Age Group: 65 years Sex: M 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 Health Status: unhealthy Age Group: 85 years Sex: F 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 Health Status: unhealthy Age Group: 86 years Sex: F 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 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 Health Status: unhealthy Age Group: 54-68 years Sex: F 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 Health Status: unhealthy Age Group: 65 years Sex: M 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 Health Status: unhealthy Age Group: 85 years Sex: F 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 Health Status: unhealthy Age Group: 86 years Sex: F Sources: https://pubmed.ncbi.nlm.nih.gov/16563066

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 2252 inducer 1087 substrate 1946	inhibitor 2438 inducer 440 substrate 1193	inhibitor 2507 substrate 1388

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 879 CYP2C19 2057	CYP3A5 446 CYP1A2 1197 CYP2A6 626 CYP2B6 776 CYP2C8 810 CYP2C19 1119 CYP2E1 729 CYP4A11 137	CYP1A2 832

Drug as perpetrator

Target	Modality	Activity
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP1A2 2333	activator 342 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP2E1 1146	activator 342 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP3A4 2633	inhibitor 4027 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 1197	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2A6 626	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2B6 776	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C19 1119	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C8 810	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C9 1193	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2D6 1388	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2E1 729	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP4A11 137	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP3A4 1946	substrate 4014 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	yes
CYP3A5 446	substrate 4014 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
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.	2007-02	17090640
Longitudinal evaluation of serum leptin and bone mineral density in early postmenopausal women.	2007-01-24	17242633
Effects of a single Silastic contraceptive implant containing nomegestrol acetate (Uniplant) on endometrial morphology and ovarian function for 1 year.	2006-12	17157108
Activation of nitric oxide synthesis in human endothelial cells using nomegestrol acetate.	2006-10	17012461
Second- and third-generation aromatase inhibitors as first-line endocrine therapy in postmenopausal metastatic breast cancer patients: a pooled analysis of the randomised trials.	2006-06-19	16736002
Characterization of related impurities in megestrol acetate.	2006-06-16	16616448
A successful live birth through in vitro fertilization program after conservative treatment of FIGO grade I endometrial cancer.	2006-06	16778408
[Pharmacological therapy of cancer anorexia-cachexia].	2006-05	16768027
Cyclic progestin administration increases energy expenditure and decreases body fat mass in perimenopausal women.	2006-04-29	16645533
Effects of estrogen, raloxifene, and hormone replacement therapy on serum C-reactive protein and homocysteine levels.	2006-02-20	15990257
Durable response of metastatic endometrial carcinoma to treatment with fulvestrant (Faslodex) after prior progestin and anastrozole therapy.	2006-02	16257043
Orchiectomy or androgen receptor blockade attenuates baroreflex-mediated bradycardia in conscious rats.	2006-01-23	16430770
Short-term progestin treatments prevent estrous induction by a GnRH agonist implant in anestrous bitches.	2006-01-20	15975646
Nanoparticles of poorly water-soluble drugs prepared by supercritical fluid extraction of emulsions.	2006-01	16307386
Letrozole: a pharmacoeconomic review of its use in postmenopausal women with breast cancer.	2006	16706574
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
Benign metastasizing leiomyoma responsive to megestrol: case report and review of the literature.	2005-12-14	16343217
New progestagens for contraceptive use.	2005-11-18	16291771
The role of aromatase inhibitors in ameliorating deleterious effects of ovarian stimulation on outcome of infertility treatment.	2005-10-04	16202169
Bleeding patterns during continuous estradiol with different sequential progestogens therapy.	2005-09-08	16145305
Progestogens: effects on clinical and biochemical parameters in postmenopausal women.	2005-09-08	16145299
[Isolation and identification of two new epimer from the mother liquid of megestrol acetate].	2005-09	16342686
Review of cost-effectiveness analyses in hormonal therapies in advanced breast cancer.	2005-09	16144501
Control of sulfatase activity by nomegestrol acetate in normal and cancerous human breast tissues.	2005-08-06	16080533
The effects of aromatase inhibitors on lipids and thrombosis.	2005-08	16100522
Bone loss and the aromatase inhibitors.	2005-08	16100521
Role of aromatase inhibitors in breast cancer.	2005-08	16100519
Nomegestrol acetate may enhance the skeletal effects of estradiol on biochemical markers of bone turnover in menopausal women after a 12-week treatment period.	2005-06	16096169
Pregnancy following intracytoplasmic sperm injection and preimplantation genetic diagnosis after the conservative management of endometrial cancer.	2005-06	15970008
Phase II study of sequential hormonal therapy with anastrozole/exemestane in advanced and metastatic breast cancer.	2005-05-09	15856035
Retrospective review of megestrol use for weight loss in an elderly veteran population.	2005-04	16548634
Effects of the combined treatment with thalidomide, megestrol and interleukine-2 in cirrhotic patients with advanced hepatocellular carcinoma. A pilot study.	2005-04	15788209
Treatment with inhibitors of angiogenesis in advanced hepatocellular carcinoma: a new tool in our hands or simply a hope?	2005-04	15788205
Antigenotoxic effects of ascorbic acid against megestrol acetate-induced genotoxicity in mice.	2005-03	15901051
Hormonal treatment of a recurrent granulosa cell tumor of the ovary: case report and review of the literature.	2005-03	15721440
[Actions of a 19-norprogesterone derivative on mammary gland: nomegestrol acetate].	2005-02	15767920
Effect of nomegestrol acetate on estrogen biosynthesis and transformation in MCF-7 and T47-D breast cancer cells.	2005-01	15748827
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
Osteoporosis associated with megestrol acetate.	2004-12	15595341
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.	2004-09	15531017
A comparison of the central effects of different progestins used in hormone replacement therapy.	2004-08-20	15283939
Serum leptin levels and body composition in postmenopausal women: effects of hormone therapy.	2004-07-10	15243285
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.	2004-06	15166617
Aromatase inhibition in the treatment of advanced breast cancer: is there a relationship between potency and clinical efficacy?	2004-05-04	15150604
Nomegestrol acetate: a progestin that deserves recognition.	2004-04	15114527
The role of MRI in the conservative management of endometrial cancer.	2004-04	15047242
Effect of nomegestrol acetate on human estrogen sulfotransferase activity in the hormone-dependent MCF-7 and T-47D breast cancer cell lines.	2004-02-26	14981909
[Nome gesrol (lutenyl) induced severe acute hepatitis].	2004-01	15041823

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)

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:47:49 GMT 2025` Edited by `admin` on `Mon Mar 31 17:47:49 GMT 2025`
Record UNII	TJ2M0FR8ES
Record Status	`Validated (UNII)`
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Name

Type

Language

MEGESTROL ACETATE

Official Name

English

MEGACE

Preferred Name

English

BDH-1298

Code

English

MEGESTROL ACETATE [USAN]

Common Name

English

MEGESTROL ACETATE [MART.]

Common Name

English

PREGNA-4,6-DIENE-3,20-DIONE, 17-(ACETYLOXY)-6-METHYL-

Systematic Name

English

SC-10363

Code

English

Megestrol acetate [WHO-DD]

Common Name

English

MEGESTROL 17.ALPHA.-ACETATE

Common Name

English

5071

Code

English

17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate

Common Name

English

MEDROXYPROGESTERONE ACETATE IMPURITY G [WHO-IP]

Common Name

English

MEGESTROL ACETATE [GREEN BOOK]

Common Name

English

MEGESTROL ACETATE [VANDF]

Common Name

English

NSC-71423

Code

English

SC 10363

Code

English

MEGESTROL ACETATE [WHO-IP]

Common Name

English

MEGESTROL ACETATE [USP-RS]

Common Name

English

MEGESTROL ACETATE [MI]

Common Name

English

MEDROXYPROGESTERONE ACETATE IMPURITY G [EP IMPURITY]

Common Name

English

6-METHYL-3,20-DIOXOPREGNA-4,6-DIEN-17-YL ACETATE [WHO-IP]

Common Name

English

BDH 1298

Code

English

MEGESTROL ACETATE [ORANGE BOOK]

Common Name

English

MEGESTEROL ACETATE

Common Name

English

MEGESTROL ACETATE [EP MONOGRAPH]

Common Name

English

MEGESTROL ACETATE [USP MONOGRAPH]

Common Name

English

Classification Tree Code System Code

EU-Orphan Drug

EU/3/17/1858