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

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

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

Molecular Formula	C22H30O3
Molecular Weight	342.4718
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
Systemic treatment of hepatocellular carcinoma.	2001	11935091
Treatment. Court decision to allow marketing of generic form of weight-loss drug.	2001 Aug 3	11548472
Serum immunoglobulins, total protein and albumin levels during UniplantR use by Nigerian women.	2001 Dec	14510101
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
Megestrol-induced Cushing syndrome.	2001 Oct	11675847
Management of common symptoms in terminally ill patients: Part I. Fatigue, anorexia, cachexia, nausea and vomiting.	2001 Sep 1	11563572
Prevention of menstruation with leuprorelin (GnRH agonist) in women undergoing myelosuppressive chemotherapy or radiochemotherapy for hematological malignancies: a pilot study.	2001 Sep-Oct	11697620
Efficacy and economics of hormonal therapies for advanced breast cancer.	2002	12149051
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
Existing and emerging endocrine therapies for breast cancer.	2002 Apr	12080538
Effects of megestrol acetate on weight gain, body composition, and pulmonary function in patients with cystic fibrosis.	2002 Apr	12006958
Fertility-preserving treatment in young patients with endometrial adenocarcinoma.	2002 Apr 15	12001117
Dronabinol versus megestrol acetate versus combination therapy for cancer-associated anorexia: a North Central Cancer Treatment Group study.	2002 Jan 15	11786587
Variant estrogen receptors and their role in liver disease.	2002 Jul 31	12161003
Effect of megestrol caproate on the reproductive function of laboratory animals.	2002 Jun	12447469
Intramuscular depot medroxyprogesterone versus oral megestrol for the control of postmenopausal hot flashes in breast cancer patients: a randomized study.	2002 Jun	12123333
[Reversal of nomegestrol acetate on multidrug resistance in drug-resistant human breast cancer cell line MCF7/ADR].	2002 Mar	12015032
Approval summary: letrozole in the treatment of postmenopausal women with advanced breast cancer.	2002 Mar	11895893
Effects of transdermal hormone replacement therapy on levels of soluble P- and E-selectin in postmenopausal healthy women.	2002 Mar	11872198
[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
Phase I and pharmacokinetic study of vinblastine and high-dose megestrol acetate.	2002 Sep	12203099
[Antigonadotropic effects of a 19-nor-progesterone derivative: the example of nomegestrol acetate].	2003 Jan	12659788
Megestrol complications.	2003 Jan	12527643
An overview of nomegestrol acetate selective receptor binding and lack of estrogenic action on hormone-dependent cancer cells.	2003 Nov	14672731
Cancer cachexia.	2003 Nov 5	14613583
Effect of nomegestrol acetate on human estrogen sulfotransferase activity in the hormone-dependent MCF-7 and T-47D breast cancer cell lines.	2003 Nov-Dec	14981909
Advances in estrogen receptor biology: prospects for improvements in targeted breast cancer therapy.	2004	14680484
A comparison of the central effects of different progestins used in hormone replacement therapy.	2004 Aug 20	15283939
Osteoporosis associated with megestrol acetate.	2004 Dec	15595341
[Nome gesrol (lutenyl) induced severe acute hepatitis].	2004 Jan	15041823
Serum leptin levels and body composition in postmenopausal women: effects of hormone therapy.	2004 Jul-Aug	15243285
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
Retrospective review of megestrol use for weight loss in an elderly veteran population.	2005 Apr	16548634
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
Hormonal treatment of a recurrent granulosa cell tumor of the ovary: case report and review of the literature.	2005 Mar	15721440
The role of aromatase inhibitors in ameliorating deleterious effects of ovarian stimulation on outcome of infertility treatment.	2005 Oct 4	16202169
Effects of a single Silastic contraceptive implant containing nomegestrol acetate (Uniplant) on endometrial morphology and ovarian function for 1 year.	2006 Dec	17157108
Durable response of metastatic endometrial carcinoma to treatment with fulvestrant (Faslodex) after prior progestin and anastrozole therapy.	2006 Feb	16257043
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
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)

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:33:23 GMT 2025` Edited by `admin` on `Mon Mar 31 17:33:23 GMT 2025`
Record UNII	EA6LD1M70M
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CHRONOPIL

Preferred Name

English

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

megestrol [INN]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QG03AC05