Pirtobrutinib (LOXO-305, LY 3527727, RXC-005) is a first-in-class, highly selective, non-covalent BTK inhibitor that inhibits multiple BTK C481 substitution mutations. Pirtobrutinib is more than 300-fold selective for BTK compared to 370 other kinases.Pirtobrutinib inhibits both wild-type BTK and BTK C481S-mediated kinase activity with nanomolar potency.Pirtobrutinib inhibits autophosphorylation of WT BTK (Y223) with an IC50 of 3.68 nM. Pirtobrutinib inhibited the autophosphorylation of WT BTK (Y223) with an IC50 of 3.68 nM. Pirtobrutinib inhibited the autophosphorylation of BTK C481S Y223, C481T Y223, and C481R Y223, with IC50s of 8.45, 7.23, and 11.73 nM, respectively.
| Molecular Weight | 479.43 |
| Formula | C22H21F4N5O3 |
| CAS Number | 2101700-15-4 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage | 2-8°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] Diana Romero. Nat Rev Clin Oncol. Initial pirtobrutinib data show promise
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NX-2127 is an orally active, potent BTK inhibitor that induces degradation of mutant BTKC481S in cells, as well as inhibits the proliferation of BTKC481S mutant TMD8 cells. In addition, NX-2127 stimulates T cell activation and increases IL-2 production in primary human T cells. |
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