Bavdegalutamide (ARV-110) is an oral, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V) and retains activity in a high androgen environment in VCaP cells.
In vivo, ARV-110 (1 mg/kg; oral gavage QD) exhibits a greater than 90% AR degradation.
| Molecular Weight | 812.29 |
| Formula | C41H43ClFN9O6 |
| CAS Number | 2222112-77-6 |
| Solubility (25°C) | DMSO 16 mg/mL |
| Storage | -20°C, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[2] Cancer Discov. Proof-of-Concept with PROTACs in Prostate Cancer
[3] Yang Wang, et al. Acta Pharm Sin B. Degradation of proteins by PROTACs and other strategies
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