Galeterone
Active Pharmaceutical Ingredients 2025-03-03
Catalog ID92689
CAS NO.851983-85-2
Purity 98%
MDL NumberMFCD16660907
EINEC Molecular FormulaC26H32N2O
Molecular Weight388.545
| Category | Content |
|---|---|
| Generic Name | Galeterone (TOK-001) |
| Chemical Formula | C26H32N2O |
| CAS Number | 851983-85-2 |
| Molecular Weight | 388.55 |
| Mechanism of Action | Galeterone is a small-molecule androgen receptor modulator and CYP17 lyase inhibitor with a triple mechanism of action:<br>1. Acts as an androgen receptor antagonist.<br>2. Inhibits CYP17 lyase, reducing androgen synthesis.<br>3. Decreases overall androgen receptor levels in prostate cancer tumors. |
| Indications | Under investigation for the treatment of castration-resistant prostate cancer (CRPC), a form of prostate cancer that progresses despite androgen deprivation therapy. |
| Clinical Trials | – Phase 1 clinical trials showed promising efficacy and tolerability in patients with CRPC.<br>- Demonstrated significant reductions in prostate-specific antigen (PSA) levels and tumor size. |
| Pharmacokinetics | – Effective at inhibiting tumor growth in preclinical models at doses of 50 mg/kg twice daily.<br>- Exhibits high oral bioavailability and significant anti-tumor effects. |
| Safety Profile | – Well-tolerated in clinical trials with no dose-limiting toxicities.<br>- Demonstrated favorable safety profile in Phase 1 studies. |
| Storage | Powder: -20°C for 3 years; In solvent: -80°C for 1 year. |
| Developer | Tokai Pharmaceuticals, Inc. |
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