Vientiane, Laos – July 14, 2024 – BigBear Pharma, a leading biopharmaceutical company focused on the development and commercialization of innovative cancer treatments, today announced that the Lao Ministry of Health has approved Adagrasib oral tablets. Adagrasib oral tablets are marketed under the brand name ADADX. Laos Registration Number: Lao Reg No.: 06L1128/24.
Adagrasib is a KRAS G12C inhibitor that irreversibly and selectively binds to KRAS G12C, locking it in an inactive state. Similar to Sotorasib, Adagrasib is a selective covalent inhibitor of KRAS G12C; however, reported differences in molecular pharmacology between the two drugs include a drug half-life of 5 hours for Sotorasib, compared to a half-life of 23 hours for Adagrasib, dose-dependent prolonged exposure for Adagrasib, and potential central nervous system penetration by Adagrasib.
Indications for Adagrasib
1. Locally Advanced or Metastatic Non-Small Cell Lung Cancer with KRAS G12C Mutation
Adagrasib (KRAZATI) as a single agent is indicated for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring a KRAS G12C mutation, as detected by an FDA-approved test, who have received at least one prior systemic therapy.
2. Locally Advanced or Metastatic Colorectal Cancer with KRAS G12C Mutation
Adagrasib (KRAZATI) in combination with cetuximab is indicated for the treatment of adult patients with locally advanced or metastatic colorectal cancer (CRC) harboring a KRAS G12C mutation, as detected by an FDA-approved test, who have received prior chemotherapy based on fluoropyrimidine, oxaliplatin, and irinotecan.
Dosage and Administration
1. Single Agent for NSCLC or Combination Therapy for CRC
600 mg orally twice daily. Take with or without food. Swallow tablets whole.
2. Missed Dose
If a dose is missed by more than 4 hours, skip that dose and resume the regular dosing schedule. If vomiting occurs, do not take a replacement dose.
Adverse Reactions
When Used as a Single Agent for Non-Small Cell Lung Cancer (NSCLC)
The most common adverse reactions (incidence ≥25%) were nausea, diarrhea, vomiting, fatigue, musculoskeletal pain, hepatotoxicity, renal impairment, edema, dyspnea, and decreased appetite.
The most common Grade 3 or 4 laboratory abnormalities (incidence ≥2%) were lymphopenia, decreased hemoglobin, increased alanine aminotransferase, increased aspartate aminotransferase, hypokalemia, hyponatremia, increased lipase, leukopenia, neutropenia, and increased alkaline phosphatase.
When Used in Combination with Cetuximab for Colorectal Cancer (CRC)
The most common adverse reactions (incidence ≥25%) were rash, nausea, diarrhea, vomiting, fatigue, musculoskeletal pain, hepatotoxicity, headache, dry skin, abdominal pain, decreased appetite, edema, anemia, and cough.
The most common Grade 3 or 4 laboratory abnormalities (incidence ≥2%) were lymphopenia, hypokalemia, hypomagnesemia, decreased hemoglobin, increased aspartate aminotransferase, increased lipase, decreased albumin, and increased alanine aminotransferase.
