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methyltestosterone

Trade name: testred

Small moleculeapproved

Approved

Dec 22, 1971

Methyltestosterone is an anabolic steroid hormone used to treat men with a testosterone deficiency. It is also used in women to treat breast cancer, breast pain, swelling due to pregnancy, and with the addition of estrogen it can treat symptoms of menopause. The effects of testosterone in humans and other vertebrates occur by way of two main mechanisms: by activation of the androgen receptor (directly or as DHT), and by conversion to estradiol and activation of certain estrogen receptors. Free testosterone (T) is transported into the cytoplasm of target tissue cells, where it can bind to the androgen receptor, or can be reduced to 5α-dihydrotestosterone (DHT) by the cytoplasmic enzyme 5α-reductase. DHT binds to the same androgen receptor even more strongly than T, so that its androgenic potency is about 2.5 times that of T. The T-receptor or DHT-receptor complex undergoes a structural change that allows it to move into the cell nucleus and bind directly to specific nucleotide sequences of the chromosomal DNA. The areas of binding are called hormone response elements (HREs), and influence transcriptional activity of certain genes, producing the androgen effects. Methyltestosterone is marketed under the brand names Android, Androral, Metandren, Oraviron, Testred, Virilon. — NCATS

Clinical trial activity

6 trials · 4 clinical orgs · 21 marketing orgs

Phase 1
1
Phase 2
5
Phase 3
0
Phase 4
0

Earliest trial started Jun 1, 2004 (NCT00141570)

Timeline

1930s

  1. Jun 1, 1936

    Evidence of US Marketing

1970s

  1. Dec 22, 1971

    Earliest FDA Approval

  2. Dec 22, 1971

    Eli Lilly — Marketing Organization

  3. Jul 24, 1972

    Inwood Laboratories — Marketing Organization

  4. Dec 3, 1973

    Bausch Health Companies — First NDA Organization

  5. Dec 3, 1973

    Bausch Health Companies — Marketing Organization

  6. Dec 3, 1973

    Bausch Health Companies — NDA Organization

  7. Jun 21, 1974

    Impax Laboratories — Marketing Organization

  8. Oct 8, 1976

    Lumara Health — Marketing Organization

  9. Feb 2, 1977

    Tablicaps — Marketing Organization

  10. Aug 3, 1979

    Schering — Marketing Organization

  11. Aug 3, 1979

    Schering-Plough — Marketing Organization

1980s

  1. Nov 5, 1982

    Lannett Company, Inc. — Marketing Organization

  2. Nov 24, 1982

    Star Pharmaceuticals — Marketing Organization

  3. Nov 24, 1982

    Chartwell Pharmaceuticals — Marketing Organization

1990s

  1. Jun 28, 1993

    Upsher-Smith Laboratories — Marketing Organization

2000s

  1. Jan 1, 2004

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2008

    Earliest Phase 1 Sponsor(trial)

2020s

  1. Feb 18, 2022

    Novitium Pharma — Marketing Organization

  2. Feb 18, 2022

    Ani Pharmaceuticals — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedDec 22, 1971
  • approvedJun 1, 1936

Chemistry & pharmacology

Loading structure…

SMILES

C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C
Mol. weight
302.451 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Oral, Topical
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

Yes

Sources

Also known as

  • 17alpha-methyl-3-oxo-4-androsten-17beta-ol
  • 17alpha-methyl-3-oxo-4-androsten-17beta-ol
  • 17(alpha)-methyl-delta(4)-androsten-17(beta)-ol-3-one
  • 17(alpha)-methyl-delta(4)-androsten-17(beta)-ol-3-one
  • 17alpha-methyl-delta(4)-androsten-17beta-ol-3-one
  • 17alpha-methyl-delta(4)-androsten-17beta-ol-3-one
  • 17alpha-methyltestosterone
  • 17alpha-methyltestosterone
  • 17-beta-hydroxy-17-methylandrost-4-en-3-one
  • 17-beta-hydroxy-17-methylandrost-4-en-3-one
  • 17beta-hydroxy-17-methylandrost-4-en-3-one
  • 17beta-hydroxy-17-methylandrost-4-en-3-one
  • 17-methyltestosteron
  • 17-methyltestosterone
  • 17-methyltestosterone
  • 17α-methyltestosterone
  • 17α-methyltestosterone
  • 17α-methyl-δ4-androsten-17β-ol-3-one
  • 17α-methyl-δ4-androsten-17β-ol-3-one
  • 4-androstene-17alpha-methyl-17beta-ol-3-one
  • 4-androstene-17alpha-methyl-17beta-ol-3-one
  • android 10
  • android 10
  • android 25
  • android 25
  • android 5
  • android 5
  • androsan
  • androsten
  • metandren
  • metandren
  • methitest
  • methitest
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosterone
  • methyltestosteronum
  • methyltestosteronum
  • metiltestosterona
  • metiltestosterona
  • nsc-9701
  • nsc-9701
  • oreton
  • oreton
  • oreton
  • oreton methyl
  • oreton methyl
  • perandren
  • perandren
  • plex hormone
  • potensan fte
  • testovis
  • testovis
  • testred
  • testred
  • virilon
  • virilon

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT04327934Phase 2Dec 1, 2017Yale University
NCT00757185Early Phase 1 (Phase 1)Feb 1, 2008John B. Pierce Laboratory, National Heart, Lung, and Blood Institute (NHLBI), Yale University
NCT00160342Phase 2Jun 1, 2005Solvay
NCT00141544Phase 2Jul 1, 2004Solvay
NCT00141557Phase 2Jul 1, 2004Solvay
NCT00141570Phase 2Jun 1, 2004Solvay
Showing 6 of 6 trials
Page 1 / 1

Organizations

Research & Development (4)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
SolvayFor profit4412004
Yale UniversityAcademic/Hospital2222008
John B. Pierce LaboratoryAcademic/Hospital1012008
National Heart, Lung, and Blood Institute (NHLBI)Government1012008
4 organizations
Page 1 / 1

Marketing (26)

OrganizationOrg typeRelationshipDate
Ani PharmaceuticalsFor profitMKTGFeb 18, 2022
Bausch Health CompaniesFor profitMKTGDec 3, 1973
Bausch Health CompaniesFor profitSYNFeb 9, 1981
Bausch Health CompaniesFor profitNDADec 3, 1973
Bausch Health CompaniesFor profitSYNDec 3, 1973
Chartwell PharmaceuticalsFor profitMKTGNov 24, 1982
Eli LillyFor profitMKTGDec 22, 1971
Heather PharmaFor profitMKTG—
Impax LaboratoriesFor profitMKTGJun 21, 1974
Impax LaboratoriesFor profitSYNSep 21, 2015
Inwood LaboratoriesFor profitMKTGJul 24, 1972
Lannett Company, Inc.For profitMKTGNov 5, 1982
Lumara HealthFor profitMKTGOct 8, 1976
MylanFor profitMKTG—
NovartisFor profitNDA2—
Novitium PharmaFor profitMKTGFeb 18, 2022
Parke-DavisFor profitMKTG—
Puracap PharmaceuticalFor profitMKTG—
ScheringFor profitMKTGAug 3, 1979
ScheringFor profitNDA2—
Schering-PloughFor profitMKTGAug 3, 1979
Star PharmaceuticalsFor profitMKTGNov 24, 1982
TablicapsFor profitMKTGFeb 2, 1977
Upsher-Smith LaboratoriesFor profitMKTGJun 28, 1993
Watson PharmaceuticalsFor profitMKTG—
West-Ward PharmaceuticalFor profitMKTG—