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megestrol

Trade name: megace

Small moleculeapproved

Approved

Aug 18, 1971

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. — NCATS

Clinical trial activity

94 trials · 110 clinical orgs · 21 marketing orgs

Phase 1
13
Phase 2
58
Phase 3
31
Phase 4
8

Earliest trial started Dec 1, 1987 (NCT00002465)

Timeline

1970s

  1. Aug 18, 1971

    Bristol-Myers — Earliest FDA Approval

  2. Aug 18, 1971

    Bristol-Myers Squibb — NDA Secondary Org

  3. Aug 18, 1971

    Bristol-Myers — NDA Organization

1980s

  1. Jan 1, 1987

    Earliest Phase 1 Sponsor(trial)

  2. Aug 8, 1988

    Par Pharmaceuticals — Marketing Organization

  3. Aug 8, 1988

    Strides Pharma Science — Marketing Organization

1990s

  1. Jan 1, 1994

    Earliest Phase 2 Sponsor(trial)

  2. Sep 29, 1995

    West-Ward Pharmaceutical — Marketing Organization

  3. Sep 29, 1995

    Hikma — Marketing Organization

  4. Nov 30, 1995

    Barr Laboratories — Marketing Organization

  5. Jan 1, 1998

    Earliest Phase 3 Sponsor(trial)

  6. Feb 27, 1998

    Teva — Marketing Organization

2000s

  1. Nov 1, 2004

    Wockhardt — Marketing Organization

  2. Nov 1, 2004

    Xttrium Laboratories — Marketing Organization

  3. Jul 5, 2005

    Endo Pharmaceuticals — NDA Secondary Org

  4. Jul 5, 2005

    Endo Pharmaceuticals — Marketing Organization

  5. Feb 16, 2006

    Apotex — Marketing Organization

  6. Feb 16, 2006

    Pharmaceutical Associates — Marketing Organization

  7. Feb 16, 2006

    Novitium Pharma — Marketing Organization

2010s

  1. Aug 27, 2014

    TWi Biotechnology, Inc. — Marketing Organization

  2. Jun 9, 2017

    Hi Tech Pharmaceuticals — Marketing Organization

  3. Jun 9, 2017

    Akorn, Inc. — Marketing Organization

  4. Dec 1, 2017

    Esteve Labs — Marketing Organization

  5. Dec 1, 2017

    Chartwell Pharmaceuticals — Marketing Organization

  6. Dec 1, 2017

    Bionpharma Inc — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedAug 18, 1971

Chemistry & pharmacology

Loading structure…

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
Mol. weight
342.4718 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • 17-acetoxy-6-methylpregna-4,6-diene-3,20-dione
  • 17-acetoxy-6-methylpregna-4,6-diene-3,20-dione
  • 17alpha-acetoxy-6-dehydro-6-methylprogesterone
  • 17alpha-acetoxy-6-dehydro-6-methylprogesterone
  • 17alpha-hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
  • 17alpha-hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
  • 17-hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate
  • 17-hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate
  • 17α-acetoxy-6-dehydro-6-methylprogesterone
  • 17α-acetoxy-6-dehydro-6-methylprogesterone
  • 17α-hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
  • 17α-hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate
  • 5071
  • 6-dehydro-6-methyl-17alpha-acetoxyprogesterone
  • 6-dehydro-6-methyl-17alpha-acetoxyprogesterone
  • 6-dehydro-6-methyl-17α-acetoxyprogesterone
  • 6-dehydro-6-methyl-17α-acetoxyprogesterone
  • 6-methyl-17alpha-acetoxypregna-4,6-diene-3,20-dione
  • 6-methyl-17alpha-hydroxy-delta(sup 6)-progesterone acetate
  • 6-methyl-17alpha-hydroxy-delta(sup 6)-progesterone acetate
  • 6-methyl-17α-acetoxypregna-4,6-diene-3,20-dione
  • 6-methyl-17α-hydroxy-delta(sup 6)-progesterone acetate
  • 6-methyl-17α-hydroxy-delta(sup 6)-progesterone acetate
  • 6-methyl-6-dehydro-17alpha-acetoxyprogesterone
  • 6-methyl-6-dehydro-17alpha-acetoxyprogesterone
  • 6-methyl-6-dehydro-17α-acetoxyprogesterone
  • 6-methyl-6-dehydro-17α-acetoxyprogesterone
  • 6-methyl-delta(sup 4,6)-pregnadien-17alpha-ol-3,20-dione acetate
  • 6-methyl-delta(sup 4,6)-pregnadien-17α-ol-3,20-dione acetate
  • 6-methyl-delta(sup 6)-dehydro-17alpha-acetoxyprogesterone
  • 6-methyl-delta(sup 6)-dehydro-17α-acetoxyprogesterone
  • apd-209
  • bdh-1298
  • bdh-1298
  • magestin
  • magestin
  • megace
  • megace
  • megace
  • megace
  • megace es
  • megace es
  • megestrol
  • megestrol
  • megestrol
  • megestrol
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestrol acetate
  • megestryl acetate
  • megstrol acetate
  • mga
  • mga
  • niagestin
  • nomegestrol acetate / estradiol
  • ovaban
  • ovaban
  • sc-10363
  • sc-10363

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07246070Phase 2Dec 31, 2025Chinese Academy of Medical Sciences, Henan Medical University
NCT07254416Phase 4Dec 15, 2025Henan Medical University, Jiao Tong University, Shaanxi Provincial People's Hospital, Shanxi Bethune Hospital, Tianjin Medical University
NCT07092137Phase 2Oct 10, 2025Guangzhou Medical University
NCT07130617Phase 1Sep 29, 2025GeneScience Pharmaceuticals Co., Ltd., Sun Yat-Sen University
NCT07243379Phase 4Sep 25, 2025GeneScience Pharmaceuticals Co., Ltd., Henan Medical University
NCT07150663Phase 3Aug 20, 2025GeneScience Pharmaceuticals Co., Ltd., Huazhong University of Science and Technology
NCT06998758Phase 3Jun 10, 2025Sun Yat-Sen University
NCT06963593Phase 4Jun 1, 2025Peking University
NCT06909383Phase 2Jun 1, 2025Guangzhou Medical University
NCT06961188Phase 3Jun 1, 2025GeneScience Pharmaceuticals Co., Ltd., Huazhong University of Science and Technology
NCT06961201Phase 3May 1, 2025GeneScience Pharmaceuticals Co., Ltd., Sichuan University
NCT06830018N/AJan 23, 2025GeneScience Pharmaceuticals Co., Ltd.
NCT06793228Phase 2Jan 15, 2025Henan Medical University
NCT06772428Phase 3Jan 1, 2025GeneScience Pharmaceuticals Co., Ltd.
NCT06549855N/AOct 31, 2024Capital Medical University, Chinese Academy of Medical Sciences, Huazhong University of Science and Technology, Peking University, Shandong University, Shengjing Hospital, Tianjin Medical University
NCT06500234Phase 3Jun 1, 2024Qingdao Central Hospital
NCT06417736N/ADec 1, 2023Zhejiang University
NCT05538897Phase 1/Phase 2 (Phase 2)Jan 13, 2023National Cancer Institute (NCI), NRG Oncology
NCT05332483Phase 1Jul 5, 2022Ontario Institute for Cancer Research, University of Toronto
NCT05316493Phase 2/Phase 3 (Phase 3)Jun 13, 2022Fudan University
Showing 20 of 94 trials
Page 1 / 5

Organizations

Research & Development (110)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government17521998
Fudan UniversityAcademic/Hospital111132013
GeneScience Pharmaceuticals Co., Ltd.For profit7742025
Henan Medical UniversityAcademic/Hospital6332014
Wake Forest UniversityAcademic/Hospital5412000
Bristol-Myers SquibbFor profit4341999
Chinese Academy of Medical SciencesAcademic/Hospital4132017
Huazhong University of Science and TechnologyAcademic/Hospital3022024
Jiao Tong UniversityAcademic/Hospital3032013
Mayo ClinicAcademic/Hospital3122000
Northwestern UniversityAcademic/Hospital3121995
Par PharmaceuticalsFor profit3322006
University of UlsanAcademic/Hospital3212011
Cancer Research UKAcademic/Hospital2022017
Endo PharmaceuticalsFor profit2222004
Guangzhou Medical UniversityAcademic/Hospital2212025
Gynecologic Oncology GroupAcademic/Hospital2222001
National Institute of Allergy and Infectious Diseases (NIAID)Government2221999
NRG OncologyAcademic/Hospital2012008
Peking UniversityAcademic/Hospital2222024
110 organizations
Page 1 / 6

Marketing (25)

OrganizationOrg typeRelationshipDate
Akorn, Inc.For profitMKTGJun 9, 2017
ApotexFor profitMKTGFeb 16, 2006
Barr LaboratoriesFor profitMKTGNov 30, 1995
Bionpharma IncFor profitMKTGDec 1, 2017
Bristol-MyersFor profitNDAAug 18, 1971
Bristol-Myers SquibbFor profitNDA2Aug 18, 1971
Chartwell PharmaceuticalsFor profitMKTGDec 1, 2017
Endo PharmaceuticalsFor profitNDA2Jul 5, 2005
Endo PharmaceuticalsFor profitMKTGJul 5, 2005
Esteve LabsFor profitMKTGDec 1, 2017
Esteve LabsFor profitSYNDec 1, 2017
Hi Tech PharmaceuticalsFor profitMKTGJun 9, 2017
HikmaFor profitMKTGSep 29, 1995
HikmaFor profitSYNSep 29, 1995
Novitium PharmaFor profitMKTGFeb 16, 2006
Par PharmaceuticalsFor profitMKTGAug 8, 1988
Pharmaceutical AssociatesFor profitMKTGFeb 16, 2006
Strides Pharma ScienceFor profitMKTGAug 8, 1988
TWi Biotechnology, Inc.For profitMKTGAug 27, 2014
TevaFor profitMKTGFeb 27, 1998
TevaFor profitSYNMay 5, 2003
Upsher-Smith LaboratoriesFor profitMKTG—
West-Ward PharmaceuticalFor profitMKTGSep 29, 1995
WockhardtFor profitMKTGNov 1, 2004
Xttrium LaboratoriesFor profitMKTGNov 1, 2004