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- Ketodarolutamide
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Ketodarolutamide | CAS No: 1297537-33-7 | GMP-certified suppliers
A medication that serves as a nonsteroidal antiandrogen targeting androgen-driven conditions such as prostate cancer, primarily intended for pharmaceutical research and development.
Therapeutic categories
Product Snapshot
- Ketodarolutamide is an oral small molecule formulation
- It is primarily investigated for use in hormone-sensitive and castration-resistant prostate cancer
- The compound is currently in the experimental stage and has not received FDA or EMA approval
Clinical Overview
Pharmacologically, ketodarolutamide functions within the class of antiandrogens, compounds that inhibit androgen receptor signaling. This mechanism is central to the therapeutic targeting of diseases driven by androgen activity, such as prostate cancer, though specific pharmacodynamic data for ketodarolutamide are not reported. The precise molecular mechanism involves antagonism of the androgen receptor, thereby preventing androgen-mediated transcriptional activation.
Key absorption, distribution, metabolism, and excretion (ADME) parameters for ketodarolutamide are not extensively characterized in publicly available data. As an active metabolite, it is derived from the parent drug darolutamide, which undergoes hepatic metabolism primarily via cytochrome P450 enzymes. The metabolic profile of ketodarolutamide likely contributes significantly to the overall antiandrogenic activity observed with darolutamide administration.
Safety and toxicity profiles for ketodarolutamide have not been fully delineated, given its experimental status and lack of clinical approval. Data from related compounds suggest that careful monitoring for class-associated adverse effects is warranted.
Currently, ketodarolutamide is not marketed under any brand names and is primarily of interest in research and development contexts. Its role as the major active metabolite of darolutamide positions it as a key contributor to the pharmacological effect of the parent drug.
For API sourcing, rigorous quality control is essential due to the compound’s experimental nature and potential use in clinical research. Suppliers should provide comprehensive documentation including purity, impurity profiles, and compliance with current Good Manufacturing Practice (GMP) standards to ensure suitability for pharmaceutical development.
Identification & chemistry
| Generic name | Ketodarolutamide |
|---|---|
| Molecule type | Small molecule |
| CAS | 1297537-33-7 |
| UNII | 9EPS75QMTL |
| DrugBank ID | DB15647 |
Pharmacology
Targets
| Target | Organism | Actions |
|---|---|---|
| Androgen receptor | Humans | antagonist |
Formulation & handling
- Ketodarolutamide is a small molecule with low water solubility, suggesting formulation challenges for aqueous delivery systems.
- Oral administration is preferred due to the solid state and physicochemical properties.
- Formulation strategies should consider enhancing bioavailability given the moderate lipophilicity and limited aqueous solubility.
Regulatory status
Ketodarolutamide is a type of Antimetabolites
Antimetabolites are a prominent category of pharmaceutical active pharmaceutical ingredients (APIs) utilized in the treatment of various diseases, particularly cancer. These compounds are structurally similar to naturally occurring metabolites essential for cellular processes such as DNA and RNA synthesis. By mimicking these metabolites, antimetabolites interfere with the normal functioning of cellular pathways, leading to inhibition of cancer cell growth and proliferation.
One of the widely used antimetabolites is methotrexate, a folic acid antagonist that inhibits the enzyme dihydrofolate reductase, disrupting the production of DNA and RNA. This disruption impedes the growth of rapidly dividing cancer cells. Another common antimetabolite is 5-fluorouracil (5-FU), which inhibits the enzyme thymidylate synthase, thereby interfering with DNA synthesis and inhibiting cancer cell proliferation.
Antimetabolites can be classified into several subcategories based on their mechanism of action and chemical structure. These include purine and pyrimidine analogs, folic acid antagonists, and pyrimidine synthesis inhibitors. Examples of antimetabolites in these subcategories include azathioprine, cytarabine, and gemcitabine.
Despite their effectiveness, antimetabolites can exhibit certain side effects due to their interference with normal cellular processes. These side effects may include gastrointestinal disturbances, myelosuppression (reduced production of blood cells), and hepatotoxicity.
In conclusion, antimetabolites are a vital category of pharmaceutical APIs used in the treatment of various diseases, especially cancer. By mimicking natural metabolites and disrupting crucial cellular processes, these compounds effectively inhibit cancer cell growth and proliferation. However, their usage should be carefully monitored due to potential side effects.
