indication
1、 Adult patients with mantle cell lymphoma (MCL) who have received at least one treatment in the past.
2、 Adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) who have received at least one treatment in the past.
effectiveness
Orelabrutinib is a BTK inhibitor. BTK is a key signaling molecule in the B cell antigen receptor (BCR) and cytokine receptor pathways, widely expressed in different types of malignant hematologic diseases, and involved in the proliferation, differentiation, and apoptosis of B cells. Obutinib inhibits the proliferation and survival of malignant B cells in vivo. This novel, potent, and highly selective BTK inhibitor is designed to target B-cell lymphoma and autoimmune indications. Compared with Imbruvica and Calquence, this drug has stronger targeting selectivity, which will improve safety.
On December 25, 2020, Orelabrutinib, a BTK inhibitor developed by Nuocheng Jianhua Company, was officially approved by the National Medical Products Administration (NMPA) of China for use in (1) adult patients with mantle cell lymphoma (MCL) who have received at least one previous treatment; (2) Adult patients with chronic lymphocytic leukemia (CLL)/small lymphocytic lymphoma (SLL) who have received at least one treatment in the past. For Nuocheng Jianhua, the approval of Obutinib is of great significance. This is the company's first innovative drug approved for market, marking the company's full entry into commercialization from clinical development.
This is the 10th original domestic small molecule kinase inhibitor approved by NMPA, the second BTK inhibitor developed by a domestic company, and the 5th BTK inhibitor launched globally. The kinase inhibitors previously approved by NMPA are: 1) Icotinib (EGFR, 2011); 2) Apatinib (VEGFR, 2014); 3) Anlotinib (VEGFR/PDGFR/KIT, 2018); 4) Pyrotinib (HER22018); 5) Fruquintinib (VEGFR, 2018); 6) Zebutinib (BTK, 2019); 7) Fumatinib Mesylate (ABL, 2019); 8) Amitinib Mesylate (EGFR-T790M, 2020); 9) Ensatinib (ALK, 2020). Currently, the FDA has approved a total of 62 small molecule kinase inhibitors.
Obutinib is an oral BTK inhibitor that irreversibly binds to BTK, inducing downstream kinase inactivation and cell death. According to the official website of Nuocheng Jianhua, the skeleton center of Obutinib is a single ring, not a fused ring. This unique structure makes Obutinib highly selective and has low non targeted side effects.
adverse reaction
Bleeding, infection, thrombocytopenia, reactivation of hepatitis B, secondary primary malignant tumor, hypertension, arrhythmia
