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 2678

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anorexia 5 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020264s017lbl.pdf	Palliative		Approved 8429	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 8429	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 1587 inducer 781 substrate 1737	inhibitor 1767 inducer 389 substrate 1037	inhibitor 1852 substrate 1217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2A6 707 CYP2C19 1478	CYP3A5 395 CYP1A2 1054 CYP2A6 543 CYP2B6 664 CYP2C8 693 CYP2C19 991 CYP2E1 667 CYP4A11 119	CYP1A2 701

Drug as perpetrator

Target	Modality	Activity
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	mild [Inhibition 50 uM]
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	moderate [Inhibition 50 uM]
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=14 Page: 14.0	no
CYP1A2 1692	activator 214 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP2E1 970	activator 214 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021778s000_ClinPharmR.pdf#page=13 Page: 13.0	yes [Activation 50 uM]
CYP3A4 1925	inhibitor 3277 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 1054	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2A6 543	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2B6 664	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C19 991	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C8 693	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2C9 1037	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2D6 1217	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP2E1 667	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP4A11 119	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	no
CYP3A4 1737	substrate 3367 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6129397/	yes
CYP3A5 395	substrate 3367 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
Managing cancer-related anorexia/cachexia.	2001	11324680
A comparison of megestrol acetate, nandrolone decanoate and dietary counselling for HIV associated weight loss.	2001 Aug	11454075
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
Effects of a short-term suspension of hormone replacement therapy on mammographic density.	2001 Sep	11532463
The impact of hormonal treatments on quality of life of patients with metastatic breast cancer.	2002	12117073
Tamoxifen resistant and refractory breast cancer: the value of aromatase inhibitors.	2002	11929341
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
[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
Postmenopausal femur bone loss: effects of a low dose hormone replacement therapy.	2003 Jul 25	12818462
Bone turnover markers and insulin-like growth factor components in metastatic breast cancer: results from a randomised trial of exemestane vs megestrol acetate.	2003 Jul-Aug	12926095
[Effects of a 19-norprogesterone derivative, the fourth decade nomegestrol acetate, on lipids].	2003 Jun	12910065
[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
Effects of progestins of human proliferative endometrium: an in vitro model of potential clinical relevance.	2003 Oct	12964029
Nomegestrol acetate: a progestin that deserves recognition.	2004 Apr	15114527
The role of MRI in the conservative management of endometrial cancer.	2004 Apr	15047242
Aromatase inhibition in the treatment of advanced breast cancer: is there a relationship between potency and clinical efficacy?	2004 May 4	15150604
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
The effects of aromatase inhibitors on lipids and thrombosis.	2005 Aug	16100522
Bone loss and the aromatase inhibitors.	2005 Aug	16100521
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
Phase II study of sequential hormonal therapy with anastrozole/exemestane in advanced and metastatic breast cancer.	2005 May 9	15856035
Benign metastasizing leiomyoma responsive to megestrol: case report and review of the literature.	2005 Nov-Dec	16343217
The role of aromatase inhibitors in ameliorating deleterious effects of ovarian stimulation on outcome of infertility treatment.	2005 Oct 4	16202169
[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
Bleeding patterns during continuous estradiol with different sequential progestogens therapy.	2005 Sep-Oct	16145305
Megestrol attenuates the hormonal response to CCK-4-induced panic attacks.	2006	16470820
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
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
Characterization of related impurities in megestrol acetate.	2006 Jun 16	16616448
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