Version July 2025
Breast cancer, metastatic (females):
Note: Although FDA approved for the secondary treatment of advancing inoperable metastatic (skeletal) mammary cancer in patients who are 1 to 5 years postmenopausal, use has been replaced by other agents. Current guidelines for the management of metastatic breast cancer do not include recommendations for the use of methyltestosterone in the treatment of this condition (Ref).
Oral: 50 to 200 mg daily.
Delayed puberty (males):
Note: Although FDA approved for the treatment of delayed puberty in males, use has been replaced by other agents. Current guidelines for the management of pubertal induction and transition to adult sex hormone replacement do not include recommendations for the use of methyltestosterone in the treatment of this condition (Ref).
Oral: 10 to 50 mg daily; limit treatment duration to 4 to 6 months; use lower range of dosing and individualize dose based on response and tolerability.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, patients with kidney disease may be at an increased risk of fluid retention.
Hepatic impairment prior to therapy: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied). However, patients with hepatic disease may be at an increased risk of fluid retention.
Hepatic impairment during therapy: Discontinue use if abnormal LFTs or cholestatic hepatitis with jaundice occur.
Refer to adult dosing. Although Beers Criteria recommends to avoid use unless indicated for hypogonadism, increased risk of liver toxicity has made methyltestosterone obsolete for this indication (Ref).
The following adverse drug reactions are derived from product labeling unless otherwise specified.
Frequency not defined:
Cardiovascular: Acute myocardial infarction, venous thromboembolism
Dermatologic: Acne vulgaris, androgenetic alopecia (male)
Endocrine & metabolic: Calcium retention, change in libido, fluid retention, gynecomastia, hirsutism, hypercholesterolemia, inhibition of gonadotropin secretion, inorganic phosphate retention, menstrual disease (including amenorrhea), potassium retention, sodium chloride retention, sodium retention
Gastrointestinal: Nausea
Genitourinary: Oligospermia (high doses), priapism, virilization (including clitoromegaly, deepening of the voice)
Hematologic & oncologic: Clotting factors suppression (factors II, V, VII, X), polycythemia
Hepatic: Abnormal hepatic function tests, cholestatic jaundice, peliosis hepatitis
Hypersensitivity: Nonimmune anaphylaxis
Nervous system: Anxiety, cerebrovascular accident, depression, headache, paresthesia
Postmarketing:
Gastrointestinal: Cholestasis (Lucey 1987)
Hepatic: Hepatocellular neoplasm (Gleeson 1991), hepatotoxicity (idiosyncratic) (Chalasani 2021), jaundice (Lucey 1987)
Men with breast cancer or with known or suspected prostate cancer; women who are or may become pregnant.
Concerns related to adverse effects:
• Cardiovascular events: Available studies are inconclusive regarding the risk of developing major adverse cardiovascular events such as nonfatal myocardial infarction, stroke, or cardiovascular death following testosterone use; most data are specific to males who were prescribed testosterone therapy (Basaria 2010; Corona 2014; Finkle 2014; Morgentaler 2015; Vigen 2013). Evaluate patients for cardiovascular risk factors prior to initiating therapy and monitor closely during therapy for cardiovascular events.
• Hepatic effects: Prolonged use and/or high doses may cause peliosis hepatis, hepatic neoplasms including hepatocellular carcinoma, cholestatic hepatitis, and jaundice. Discontinue if cholestatic hepatitis with jaundice or abnormal liver function tests occur.
• Oligospermia: May cause oligospermia and reduced ejaculatory volume after prolonged administration or excessive dosage.
• Polycythemia: May increase hematocrit requiring dose adjustment or discontinuation. Withhold initial treatment in patients with hematocrit >48% or >50% if living at higher altitudes. Discontinue therapy if hematocrit exceeds 54% (ES [Bhasin 2018]).
• Priapism: Priapism or excessive sexual stimulation may occur.
• Venous thromboembolism: Venous thromboembolic events, including deep vein thrombosis (DVT) and pulmonary embolism (PE), have been reported with testosterone products. Evaluate patients with symptoms of pain, edema, warmth, and erythema in the lower extremity for DVT and those with acute shortness of breath for PE. Discontinue therapy if a venous thromboembolism is suspected. Use in patients with thrombophilia is not recommended (ES [Bhasin 2018]).
Disease-related concerns:
• Benign prostatic hyperplasia: Androgens may worsen benign prostatic hyperplasia (BPH); do not use in patients with severe lower urinary tract symptoms (American Urological Association/International Prostate Symptom Score >19) (ES [Bhasin 2018]). Discontinue therapy if urethral obstruction develops in patients with BPH (use lower dose if restarted).
• Breast cancer: May cause hypercalcemia (by stimulating osteolysis) in patients with breast cancer; discontinue if hypercalcemia occurs.
• Diseases exacerbated by fluid retention: Use with caution in patients with diseases that may be exacerbated by fluid retention, including cardiac impairment; may cause fluid retention.
• Hepatic impairment: Use with caution in patients with hepatic impairment; may cause fluid retention.
• Prostate cancer: May increase the risk of prostate cancer. Withhold therapy pending urological evaluation in patients with palpable prostate nodule or induration, PSA >4 ng/mL, or PSA >3 ng/mL in patients at high risk of prostate cancer (ES [Bhasin 2018]).
• Renal impairment: Use with caution in patients with renal impairment; may cause fluid retention.
• Sleep apnea: May potentiate sleep apnea in some male patients, especially those with risk factors (eg, obesity, chronic lung disease). Withhold initial treatment in patients with untreated obstructive sleep apnea (ES [Bhasin 2018]).
Special populations:
• Females: During treatment for metastatic breast cancer, females should be monitored for signs of virilization (eg, deepening of voice, hirsutism, acne, clitoromegaly, menstrual irregularities); discontinue if mild virilization is present to prevent irreversible symptoms.
• Pediatric: May accelerate bone maturation (without producing compensatory gain in linear growth) and premature closure of the epiphyses in children; in prepubertal children, perform radiographic examination of the hand and wrist every 6 months to determine the rate of bone maturation and to assess the effect of treatment on the epiphyseal centers. Use with caution in males with delayed puberty.
Other warnings/precautions:
• Abuse/misuse/diversion: Anabolic steroids may be abused, typically at doses higher than recommended and in combination with other anabolic androgenic steroids; abuse may be associated with serious cardiovascular and psychiatric adverse reactions. Inform patients of the serious adverse reactions associated with abuse of testosterone and anabolic androgenic steroids; if abuse is suspected, check serum testosterone levels (testosterone levels may be in the normal or subnormal range in males abusing synthetic testosterone derivatives). Consider the possibility of abuse in suspected patients who present with serious cardiovascular or psychiatric adverse events.
• Dependence: Drug dependence in individuals using approved doses of testosterone for approved indications has not been documented; however, dependence may occur when used outside of approved dosage/indications.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Generic: 10 mg
Tablet, Oral:
Methitest: 10 mg [scored]
Yes
Capsules (methylTESTOSTERone Oral)
10 mg (per each): $83.89
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C-III
Administer orally.
Hazardous agent (NIOSH 2024 [table 2]).
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2023; NIOSH 2024; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Breast cancer, metastatic (females): Secondarily in females with advancing inoperable metastatic (skeletal) mammary cancer who are 1 to 5 years postmenopausal; has also been used in premenopausal females with breast cancer who have benefited from oophorectomy and are considered to have a hormone-responsive tumor.
Note: Although FDA approved for the secondary treatment of advancing inoperable metastatic (skeletal) mammary cancer in patients who are 1 to 5 years postmenopausal, use has been replaced by other agents. Current guidelines for the management of metastatic breast cancer do not include recommendations for the use of methyltestosterone in the treatment of this condition (ASCO [Rugo 2016]; ESMO [Gennari 2021]).
Delayed puberty (males): To stimulate puberty in carefully selected males with clearly delayed puberty.
Note: Although FDA approved for the treatment of delayed puberty in males, use has been replaced by other agents. Current guidelines for the management of pubertal induction and transition to adult sex hormone replacement do not include recommendations for the use of methyltestosterone in the treatment of this condition (Endo-ERN [Nordenström 2022]).
MethylTESTOSTERone may be confused with medroxyPROGESTERone, methylPREDNISolone
Beers Criteria: Methyltestosterone is identified in the Beers Criteria as a potentially inappropriate medication to be avoided in patients 65 years of age and older due to its potential for cardiac problems and potential risks in men with prostate cancer (Beers Criteria [AGS 2023]).
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.
Agents with Blood Glucose Lowering Effects: Androgens may increase hypoglycemic effects of Agents with Blood Glucose Lowering Effects. Risk C: Monitor
Ajmaline: Androgens may increase adverse/toxic effects of Ajmaline. Specifically, the risk for cholestasis may be increased. Risk C: Monitor
C1 Inhibitors: Androgens may increase thrombogenic effects of C1 Inhibitors. Risk C: Monitor
Corticosteroids (Systemic): May increase fluid-retaining effects of Androgens. Risk C: Monitor
CycloSPORINE (Systemic): Androgens may increase hepatotoxic effects of CycloSPORINE (Systemic). Androgens may increase serum concentration of CycloSPORINE (Systemic). Management: Consider avoiding concomitant use of androgens and cyclosporine. If concomitant use is unavoidable, monitor serum cyclosporine concentrations and for signs and symptoms of hepatotoxicity. Cyclosporine dose reductions may be required. Risk D: Consider Therapy Modification
Hypertension-Associated Agents: May increase hypertensive effects of Androgens. Risk C: Monitor
Vitamin K Antagonists: Androgens may increase anticoagulant effects of Vitamin K Antagonists. Management: Monitor for increased effects of vitamin K antagonists if an androgen is initiated/dose increased, or decreased effects if androgen is discontinued/dose decreased. Significant reductions in vitamin K antagonist dose are likely required. Risk D: Consider Therapy Modification
Use is contraindicated in females who may become pregnant. Use of methyltestosterone may impair fertility; oligospermia may occur in males and amenorrhea may occur in females.
Use is contraindicated in females who are pregnant. Exposure during pregnancy may cause virilization of the external genitalis of the female fetus, including clitoromegaly, abnormal vaginal development, and fusion of genital folds to form a scrotal-like structure. The degree of masculinization is dose related and most likely to occur when androgens are administered in the first trimester. If a patient becomes pregnant while taking androgens, counsel on the potential hazard to the fetus.
It is not known if methyltestosterone is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother.
LFTs, lipid panel, hemoglobin and hematocrit (at 3 to 6 months then annually). Monitor urine and serum calcium and signs of virilization in females treated for breast cancer. Serum glucose (may be decreased by testosterone, monitor patients with diabetes). Monitor for cardiovascular events closely during therapy. Monitor PSA if clinically indicated. In prepubertal patients, perform radiologic examination of wrist and hand every 6 months.
Endogenous androgen stimulates receptors in organs and tissues to promote growth and development of male sex organs and maintains secondary sex characteristics in androgen-deficient males
Protein binding: 98% bound to sex hormone-binding globulin
Metabolism: Hepatic
Half-life elimination: Variable: 10 to 100 minutes
Excretion: Urine (~90%); feces (~6%)
