The functions, efficacy and side effects of adagrasib

Adagrasib (Adagrasib) is a targeted therapy for non-small cell lung cancer (NSCLC) and colorectal cancer (CRC) with KRAS G12C gene abnormalities. Adagrasib reduces tumor growth by locking the KRAS protein in an inactive state.

As an irreversible inhibitor of KRAS G12C, adagrasib can form a covalent bond with the mutated cysteine in KRAS G12C, thereby stabilizing the mutated KRAS protein in an inactive state. This mechanism effectively blocks the transmission of downstream signals without interfering with wild-type KRAS protein. In this way, adagrasib inhibits tumor growth and cell viability in cells carrying KRAS G12C mutations, thereby achieving tumor regression in KRAS G12C-mutated tumor xenograft models, while exhibiting minimal off-target activity in the process.

AdagrasiibNCSLC Monotherapy: The most common adverse reactions (≥ 25%) were nausea, diarrhea, vomiting, fatigue, musculoskeletal pain, hepatotoxicity, renal impairment, edema, dyspnea, and decreased appetite. The most common (≥2%) grade 3 or 4 laboratory abnormalities were lymphopenia, decreased hemoglobin, increased alanine aminotransferase, increased aspartate aminotransferase, hypokalemia, hyponatremia, increased lipase, leukopenia, neutropenia, and increased alkaline phosphatase.

Adagrasiib combined with cetuximab for the treatment of colorectal cancer: The most common adverse reactions (≥25%) are rash, nausea, diarrhea, vomiting, fatigue, musculoskeletal pain, hepatotoxicity, headache, dry skin, abdominal pain, decreased appetite, edema, anemia, and cough. The most common (≥2%) grade 3 or 4 laboratory abnormalities were lymphopenia, decreased potassium, decreased magnesium, decreased hemoglobin, increased aspartate aminotransferase, increased lipase, decreased albumin, and increased alanine aminotransferase.

It should be noted that the above-mentioned side effects may occur, but not all patients will experience them, and the severity of side effects varies from individual to individual. Therefore, during the use of adagrasib, patients should closely observe their own reactions and communicate with their doctors in a timely manner for effective treatment.