TSR-011 is an orally available ALK inhibitor being developed for the treatment of solid tumors including NSCLC. ALK is known to be involved in certain types of cancers, including subsets of non-small cell lung cancer, neuroblastoma and lymphoma. TSR-011 is a potent inhibitor of both anaplastic lymphoma kinase (ALK) and tropomyosin-related kinases (TRK). Preliminary results after eight weeks of treatment with TSR-011 demonstrated disease control (partial responses plus stable disease) in 11 of 17 (65%) evaluable patients treated with TSR-011.
| Molecular Weight | 577.73 |
| Formula | C33H44FN5O3 |
| CAS Number | 1357920-84-3 |
| Solubility (25°C) | 100 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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] Yekaterina B Khotskaya, et al. Targeting TRK family proteins in cancer
[4] Georg Pall. The next-generation ALK inhibitors
[5] Mark M Awad, et al. ALK inhibitors in non-small cell lung cancer: crizotinib and beyond
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