Methyltestosterone

Androgen — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Methyltestosterone is an ofp drug in the Androgen class catalogued in DrugCentral. It was first approved by the FDA in 1973. Its mechanism of action is classified as Androgen Receptor Agonists. DrugCentral lists 5 molecular targets, including AR, SHBG and Ar. Recorded indications include Bilateral Anorchia, Deficiency of testosterone biosynthesis, Delayed puberty and Hormone receptor positive malignant neoplasm of breast.

• Approval status: ofp (first approved 1973 by the FDA).
• Drug class: Androgen.
• Mechanism of action: Androgen Receptor Agonists.
• Molecular targets: AR, SHBG, Ar and PGR (5 listed in DrugCentral).
• Indications: Bilateral Anorchia, Deficiency of testosterone biosynthesis, Delayed puberty, Hormone receptor positive malignant neoplasm of breast and Inhibition of lactation procedure and others.
• ATC code: G03BA02 (3-oxoandrosten (4) derivatives).
• Molecular formula: C20H30O2; molecular weight 302.46 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (10)

• Bilateral Anorchia
• Deficiency of testosterone biosynthesis
• Delayed puberty
• Hormone receptor positive malignant neoplasm of breast
• Inhibition of lactation procedure
• LHRH Deficiency
• Male hypogonadism
• Menopausal flushing
• Primary Hypogonadism due to Bilateral Torsion
• Primary Hypogonadism due to Orchitis

Off-label uses (3)

• Klinefelter's syndrome, XXY
• Noonan's syndrome
• Undescended testicle

Contraindications (53)

• Asthma
• Benign prostatic hyperplasia
• Body fluid retention
• Breast Carcinoma in Males
• Breast lump
• Breastfeeding (mother)
• Carcinoma of female breast
• Cardiovascular event risk
• Cerebrovascular accident
• Chloasma
• Chorea
• Deep venous thrombosis
• Dementia
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Disorder of gallbladder
• Edema
• Endometrial carcinoma
• Endometriosis
• Epilepsy
• Estrogen receptor positive tumor
• Family history of malignant neoplasm of breast
• Functional visual loss
• Heart failure
• Hepatic porphyria
• Humoral hypercalcemia of malignancy
• Hypercalcemia
• Hypercholesterolemia
• Hyperlipoproteinemia
• + 23 more

Mechanism & targets

• Mechanism of action (MoA): Androgen Receptor Agonists
• Established pharmacologic class: Androgen

Molecular targets (5)

Target	Gene	Action	Activity
Androgen receptor	AR	agonist	EC50 9.66
Sex hormone-binding globulin	SHBG	unknown	Kd 8.43
Androgen receptor	Ar	unknown	IC50 7.80
Progesterone receptor	PGR	unknown	Ki 7.48
Glucocorticoid receptor	NR3C1	unknown	Ki 6.08

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1973-12-03	FDA	—	VALEANT PHARM INTL

ATC classification

ATC code	Therapeutic hierarchy
G03BA02	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ANDROGENS › 3-oxoandrosten (4) derivatives
G03EA01	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION › Androgens and estrogens
G03EK01	GENITO URINARY SYSTEM AND SEX HORMONES › SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM › ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION › Androgens and female sex hormones in combination with other drugs

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Intracranial pressure increased	36.4
Urticaria pressure	33.3

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Methyltestosterone is on its molecule page.

• Molecular formula: C₂₀H₃₀O₂
• Molecular weight: 302.46 g/mol
• CAS number: 58-18-4
• InChIKey: GCKMFJBGXUYNAG-HLXURNFRSA-N
• PubChem CID: 6010

C[C@]1(O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Methyltestosterone used for?

DrugCentral lists the following indications for Methyltestosterone: Bilateral Anorchia, Deficiency of testosterone biosynthesis, Delayed puberty, Hormone receptor positive malignant neoplasm of breast, Inhibition of lactation procedure, LHRH Deficiency, Male hypogonadism and Menopausal flushing and others.

How does Methyltestosterone work?

Methyltestosterone is classified as Androgen Receptor Agonists; its molecular targets in DrugCentral include AR (agonist), SHBG, Ar and PGR.

When was Methyltestosterone first approved?

Methyltestosterone was first approved by the FDA in 1973.

What drug class does Methyltestosterone belong to?

Methyltestosterone is in the Androgen class.

What is the chemical formula of Methyltestosterone?

Methyltestosterone has the molecular formula C20H30O2 and a molecular weight of 302.46 g/mol.

Sources

• DrugCentral drug card 3356 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1395 — compound record and bioactivity
• PubChem CID 6010 — chemical identifiers
• DrugBank DB06710 — drug record
• FDA UNII V9EFU16ZIF — substance identity
• DailyMed: FDA labels for Methyltestosterone — current prescribing information (label search)
• UniProt P10275 (AR) — target protein
• UniProt P04278 (SHBG) — target protein
• UniProt P04150 (NR3C1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.