Oritinib mesylate  (Synonyms: SH-1028 mesylate)

Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC₅₀ of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation^[1].

Oritinib (SH-1028) (72 hours; 10 μmol/L and the 3-fold dilution; nine times) mesylate selectively inhibits EGFR-mutated NCI-H1975, H3255 and PC-9 cells, with IC₅₀ values of 3.93, 9.39 and 7.63 nM, respectively, which is more sensitive than the inhibition of wild-type EGFR in A431 cells^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate inhibits EGFR-mutant tumor progression but not wild-type EGFR in vivo^[1].
Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate only induces a moderate tumor growth inhibition in A431 (wild-type EGFR) tumor xenografts, while causes profound and sustained tumor shrinkage in both NCI-H1975 and PC-9 xenograft models with EGFR mutations with 5 mg/kg/day^[1].
Oritinib (SH-1028) (p.o.; once daily for consecutive 14 days; 2.5-15 mg/kg) mesylate shows good bioavailability, and is distributed extensively from the plasma to the tissues with T_max of 1.5-2 h, and AUC_0–t values of SH-1028 in plasma are 118, 300 and 931 ng × h/ml on Day 1, while 272, 308 and 993 ng × h/ml on Day 14^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

635.78

C₃₂H₄₁N₇O₅S

2180164-79-6

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• [1]. Han L, et al. SH-1028, An Irreversible Third-Generation EGFR TKI, Overcomes T790M-Mediated Resistance in Non-Small Cell Lung Cancer. Front Pharmacol. 2021;12:665253.  [Content Brief]