Boronic acids and boronate esters are commonly used reagents in Suzuki–Miyaura coupling chemistry. Organoboron derivatives are common reagents for C–C bond formation, either through classical palladium-mediated transformations or through other newer coupling methods. Boronic esters and acids are potential intermediates in the manufacture of many active pharmaceutical ingredients (API).
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Dec. 26, 2023, Amgen announced that the U.S. FDA has completed its review of the company's supplemental New Drug Application seeking full approval of LUMAKRAS (sotorasib).
LUMAKRAS (sotorasib) is an oral, first-in-class therapy indicawithted for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC) following at least one previous systemic therapy.
Sotorasib is the first approved targeted therapy for patients with tumors with any KRAS mutation, which accounts for approximately 25% of mutations in NSCLC. The U.S. FDA granted the application for sotorasib orphan drug, fast track, priority review, and breakthrough therapy designations.
On January 20, Jacobio Pharma presents data of glecirasib in patients with pancreatic cancer and other solid tumors at the 2024 ASCO GI. For second-line and above KRAS G12C mutated pancreatic cancer patients, the confirmed objective response rate (cORR) was 41.9% and the disease control rate (DCR) was 93.5%. Glecirasib is a potential best-in-class KRAS G12C allosteric inhibitor with promising early clinical efficacy. Glecirasib can be used as monotherapy to treat non-small cell lung cancer, colorectal cancer and other solid tumors with the KRAS G12C mutation. Combinations of Glecirasib with SHP2i, EGFRi, or PD-1 antibodies is expected to have synergistic efficacy and overcome acquired drug resistance.
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