Stereochemistry | ABSOLUTE |
Molecular Formula | C26H32N2O |
Molecular Weight | 388.5451 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC=C(N3C=NC4=C3C=CC=C4)[C@@]1(C)CC[C@@]5([H])[C@@]2([H])CC=C6C[C@@H](O)CC[C@]56C
InChI
InChIKey=PAFKTGFSEFKSQG-PAASFTFBSA-N
InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1
Molecular Formula | C26H32N2O |
Molecular Weight | 388.5451 |
Charge | 0 |
Count |
MOL RATIO
1 MOL RATIO (average) |
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 6 / 6 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Galeterone (TOK-001, formerly called VN/124-1) is a potent anti-androgen with three modes of action. The compound acts as a specific androgen receptor antagonist, inhibits CYP17 lyase while conserving CYP17 hydroxylase function, and decreases overall androgen receptor levels in prostate cancer cells. Galeterone is a first in class, multi-targeted small-molecule drug that disrupts the growth and survival of prostate cancer cells. Tokai Pharmaceuticals is developing galeterone as an oral treatment for castration-resistant prostate cancer. Phase III clinical development of galeterone is underway in the US, Canada, Australia, Western Europe, Spain and the United Kingdom.
Originator
Approval Year
Sourcing
PubMed
Patents
Sample Use Guides
A once-daily galeterone dose of 2550mg was recommended for use in patients with castration-resistant prostate cancer based on results from part 1 of the phase II trial.
Route of Administration:
Oral