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- Methyltestosterone
Testosteronum (Methyltestosterone) API Manufacturers & Suppliers
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Methyltestosterone | CAS No: 58-18-4 | GMP-certified suppliers
A medication that treats testosterone deficiency in men and manages breast cancer, breast pain, pregnancy-related swelling, and menopausal symptoms in women through androgen replacement therapy.
Therapeutic categories
Primary indications
- 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
Product Snapshot
- Methyltestosterone is available as an oral small molecule in various tablet and capsule formulations
- It is primarily utilized for testosterone deficiency treatment in males and adjunctive use in certain female breast conditions and menopausal symptom management
- The drug is approved for use in the US and Canadian markets
Clinical Overview
Pharmacologically, methyltestosterone belongs to the class of androgens and derivatives, specifically 3-hydroxylated C19 steroid hormones. These compounds regulate the development and maintenance of male secondary sexual characteristics and exert notable effects on hair growth patterns on the scalp and body. Endogenous testosterone, the natural analogue, is primarily secreted by the testes in males and produced in smaller amounts in females by the ovaries, adrenal glands, and peripheral conversion. Testosterone modulates multiple physiological processes including libido, energy metabolism, immune function, and bone density maintenance.
The mechanism of action involves methyltestosterone’s interaction with androgen receptors in target tissues. The drug enters the cytoplasm of cells where it may bind directly to androgen receptors or be enzymatically converted to 5α-dihydrotestosterone (DHT) by 5α-reductase. DHT possesses a higher binding affinity, approximately 2.5-fold greater than testosterone, enhancing androgenic effects. The receptor-ligand complex translocates to the cell nucleus, binding to hormone response elements (HREs) on DNA, thereby modulating gene transcription and eliciting androgenic and anabolic responses.
Key ADME parameters include metabolism primarily mediated by cytochrome P450 enzymes, notably CYP3A4 and CYP2B6 isoforms. It exhibits a pattern of renal excretion. Safety considerations emphasize the potential for virilization, hepatotoxicity, cardiovascular risks, and endocrine suppression with prolonged use. Monitoring is essential during treatment, especially given the Schedule III classification indicating controlled access due to abuse potential.
Notable pharmaceutical formulations of methyltestosterone exist globally, with diverse dosing regimens adapted to clinical contexts ranging from endocrine disorders to adjunctive oncologic therapy.
For API sourcing, attention to pharmacopeial standards, impurity profiles, and batch-to-batch consistency is critical. Due to its controlled status, regulatory compliance for procurement and documentation is mandatory. Suppliers should provide comprehensive certificates of analysis and demonstrate adherence to GMP to ensure quality and traceability for pharmaceutical manufacture.
Identification & chemistry
| Generic name | Methyltestosterone |
|---|---|
| Molecule type | Small molecule |
| CAS | 58-18-4 |
| UNII | V9EFU16ZIF |
| DrugBank ID | DB06710 |
Pharmacology
| Summary | Methyltestosterone acts primarily by activating androgen receptors directly or via its metabolite dihydrotestosterone (DHT), leading to modulation of gene transcription through hormone response elements. It also undergoes aromatization to estradiol, which activates estrogen receptor alpha, contributing to its biological effects. Therapeutically, it functions as an anabolic steroid hormone to address testosterone deficiency and certain estrogen-responsive conditions. |
|---|---|
| Mechanism of action | 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. |
| Pharmacodynamics | Testosterone is a steroid hormone from the androgen group. Testosterone is primarily secreted from the testes of males. In females, it is produced in the ovaries, adrenal glands and by conversion of adrostenedione in the periphery. It is the principal male sex hormone and an anabolic steroid. In both males and females, it plays key roles in health and well-being. Examples include enhanced libido, energy, immune function, and protection against osteoporosis. On average, the adult male body produces about twenty times the amount of testosterone than an adult female's body does. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Androgen receptor | Humans | agonist |
| Estrogen receptor alpha | Humans |
ADME / PK
| Absorption | The methyl group aids to increase oral bioavailability. |
|---|---|
| Half-life | 6-8 hours |
| Protein binding | 40% of testosterone in plasma is bound to sex hormone-binding globulin and 2% remains unbound and the rest is bound to albumin and other proteins. |
| Metabolism | Hepatic. Testosterone is metabolized to 17-keto steroids through two different pathways. The major active metabolites are estradiol and dihydrotestosterone (DHT). |
| Route of elimination | 90% urine / 10% feces |
Formulation & handling
- Methyltestosterone is a small molecule androgen primarily formulated for oral administration in tablet or capsule forms.
- Its low water solubility and moderate lipophilicity (LogP 3.65) may necessitate formulation strategies to enhance bioavailability.
- As a steroidal compound, it is chemically stable under standard handling conditions but requires protection from moisture and light to maintain potency.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has patent protection expired in both the US and Canada, allowing for generic competition. Consequently, the products are at a mature stage of the market lifecycle in these regions. |
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| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Methyltestosterone includes multiple originator companies producing branded formulations such as Android, Covaryx, and Eemt for the US and Canadian markets. These branded products have established presence primarily in North America with no significant penetration reported in EU or other regions. Patent expirations indicate the presence of existing generic competition in these markets. |
|---|
Safety
| Toxicity | Side effects include amnesia, anxiety, discolored hair, dizziness, dry skin, hirsutism, hostility, impaired urination, paresthesia, penis disorder, peripheral edema, sweating, and vasodilation. |
|---|
- Handle with appropriate protective equipment to avoid dermal absorption, as exposure may cause skin dryness and hirsutism
- Use in well-ventilated areas to minimize inhalation risk, considering potential systemic effects such as dizziness and paresthesia
- Avoid contamination to prevent unintended exposure that could lead to vasodilation and peripheral edema
Methyltestosterone is a type of Androgens
Androgens are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in hormone replacement therapy and various other medical applications. They are a class of hormones that primarily include testosterone and its derivatives, which are responsible for the development and maintenance of male characteristics in the body.
Androgens are commonly used in the treatment of conditions such as hypogonadism, delayed puberty, androgen deficiency syndromes, and certain types of breast cancer. They work by binding to and activating the androgen receptors in cells, regulating gene expression and influencing the development and functioning of various tissues and organs.
Pharmaceutical companies produce androgens as API compounds to ensure precise dosage and efficacy in pharmaceutical formulations. These APIs undergo rigorous testing and quality control measures to meet regulatory standards and ensure patient safety.
The availability of androgens as APIs enables the formulation of different dosage forms such as tablets, injections, gels, and transdermal patches. These formulations provide healthcare professionals with various options for administration, allowing them to tailor treatment regimens according to individual patient needs.
It is essential for pharmaceutical companies to maintain strict quality control and adhere to Good Manufacturing Practices (GMP) during the production of androgens APIs. This ensures consistent potency, purity, and bioavailability of the APIs, ultimately leading to safe and effective medications for patients.
In conclusion, androgens are a vital subcategory of pharmaceutical APIs used in hormone replacement therapy and the treatment of various medical conditions. Their precise production and formulation allow for effective therapeutic interventions, promoting optimal patient outcomes.
Methyltestosterone (Androgens), classified under Hormonal Agents
Hormonal agents are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) widely used in the medical field. These substances play a crucial role in regulating and modulating hormonal functions within the body. Hormonal agents are designed to mimic or manipulate the effects of naturally occurring hormones, allowing healthcare professionals to treat various endocrine disorders and hormonal imbalances.
Hormonal agents are commonly employed in the treatment of conditions such as hypothyroidism, hyperthyroidism, diabetes, and hormonal cancers. These APIs work by interacting with specific hormone receptors, either by stimulating or inhibiting their activity, to restore the balance of hormones in the body. They can be administered orally, intravenously, or through other routes depending on the specific medication and patient needs.
Pharmaceutical companies employ rigorous manufacturing processes and quality control measures to ensure the purity, potency, and safety of hormonal agent APIs. These APIs are synthesized using chemical or biotechnological methods, often starting from natural hormone sources or through recombinant DNA technology. Stringent regulatory guidelines are in place to guarantee the efficacy and safety of hormonal agent APIs, ensuring that patients receive high-quality medications.
As the demand for hormone-related therapies continues to grow, ongoing research and development efforts focus on enhancing the effectiveness and reducing the side effects of hormonal agent APIs. This includes the exploration of novel delivery systems, advanced formulations, and targeted drug delivery methods. By continuously advancing our understanding and capabilities in hormonal agents, the medical community can improve patient outcomes and quality of life for individuals with hormonal disorders.
