adagrasib

Also Known As:

2-((S)-4-(7-(8-chloronaphthalen-1-yl)-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-5,6,7,8-tetrahydropyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoroacryloyl)piperazin-2-yl)acetonitrile; 2-piperazineacetonitrile, 4-(7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-(((2S)-1-methyl-2-pyrrolidinyl)methoxy)pyrido(3,4-d)pyrimidin-4-yl)-1-(2-fluoro-1-oxo-2-propen-1-yl)-, (2S)-; MRTX-849; MRTX849

Networked: 68 relevant articles (7 outcomes, 18 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Experts

1.	Christensen, James G: 8 articles (10/2022 - 01/2020)
2.	Olson, Peter: 6 articles (01/2022 - 01/2020)
3.	Johnson, Melissa L: 4 articles (10/2022 - 01/2020)
4.	Jänne, Pasi A: 4 articles (10/2022 - 01/2020)
5.	Briere, David M: 4 articles (01/2022 - 01/2020)
6.	Hallin, Jill: 4 articles (01/2022 - 01/2020)
7.	Heist, Rebecca S: 4 articles (01/2022 - 01/2021)
8.	Sudhakar, Niranjan: 4 articles (01/2022 - 01/2020)
9.	Chao, Richard C: 3 articles (10/2022 - 01/2020)
10.	Rybkin, Igor I: 3 articles (10/2022 - 01/2020)

Related Diseases

1.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 01/01/2021 - "KRASG12C inhibitors, including MRTX849, are promising treatment options for KRAS-mutant non-small cell lung cancer (NSCLC). " 11/01/2022 - "The KRYSTAL-1 study of adagrasib - a new trial for KRASG12C-mutated non-small-cell lung cancer." 01/01/2022 - "In the phase II KRYSTAL-1 trial, the KRASG12C inhibitor adagrasib yielded an overall response rate of 43% and a disease control rate of 80% in patients with previously treated KRASG12C-mutant non-small cell lung cancer. " 01/01/2024 - "First Approval of Adagrasib for the Treatment of Non-Small Cell Lung Cancer Harboring a KRASG12C Mutation." 11/01/2023 - "According to the latest update from KRYSTAL-1, adagrasib shows durable efficacy in patients with advanced, previously treated KRASG12C non-small cell lung cancer. "
2.	Neoplasms (Cancer) 05/01/2023 - "Clinical trials have shown that adagrasib causes cancer reduction or resolution in 42.9% of people with NSCLC with KRASG12C mutations who receive the drug. " 01/01/2023 - "In this phase II cohort of the KRYSTAL-1 study (ClinicalTrials.gov identifier: NCT03785249; phase Ib cohort), we evaluated adagrasib (600 mg orally twice daily) in patients with KRASG12C-mutated advanced solid tumors (excluding NSCLC and CRC). " 10/31/2023 - "In this work, we explore the ability of MRTX1257, a KRASG12C inhibitor analogous to MRTX849, to radio-sensitize KRASG12C+/+ mutated cell lines and tumors. " 10/01/2023 - "Tumor ABCB1 overexpression may thus confer adagrasib resistance. " 01/01/2023 - "Adagrasib demonstrates encouraging clinical activity and is well tolerated in this rare cohort of pretreated patients with KRASG12C-mutated solid tumors."
3.	Neoplasm Metastasis (Metastasis) 10/01/2023 - "We evaluated adagrasib in patients with KRASG12C-mutated NSCLC and untreated CNS metastases from the KRYSTAL-1 trial (ClinicalTrials.gov identifier: NCT03785249; phase Ib cohort), in which adagrasib 600 mg was administered orally, twice daily. " 10/01/2023 - "Adagrasib is the first KRASG12C inhibitor to prospectively demonstrate IC activity in patients with KRASG12C-mutated NSCLC and untreated CNS metastases, supporting further investigation in this population." 10/01/2023 - "Intracranial Efficacy of Adagrasib in Patients From the KRYSTAL-1 Trial With KRASG12C-Mutated Non-Small-Cell Lung Cancer Who Have Untreated CNS Metastases." 01/01/2023 - "As of September 1, 2022, a total of 853 patients with KRASG12C-mutated solid tumors, including patients with CNS metastases, had received adagrasib (monotherapy or in combination). "
4.	Colorectal Neoplasms (Colorectal Cancer) 10/31/2023 - "Among them, MRTX849 (Mirati Therapeutics) showed encouraging clinical outcomes for the treatment of selected patients with KRASG12C mutated NSCLC and colorectal cancers. " 01/01/2023 - "Adagrasib, a KRASG12C inhibitor, has demonstrated clinical activity in patients with KRASG12C-mutated non-small-cell lung cancer (NSCLC) and colorectal cancer (CRC). " 11/01/2021 - "In phase I/II KRYSTAL-1 trial, the KRASG12C inhibitor adagrasib demonstrated encouraging clinical activity against metastatic colorectal cancer, both as a monotherapy and when combined with the EGFR inhibitor cetuximab. " 01/01/2023 - "Adagrasib had antitumor activity in heavily pretreated patients with metastatic colorectal cancer with mutant KRAS G12C, both as oral monotherapy and in combination with cetuximab. " 01/01/2023 - "In this phase 1-2, open-label, nonrandomized clinical trial, we assigned heavily pretreated patients with metastatic colorectal cancer with mutant KRAS G12C to receive adagrasib monotherapy (600 mg orally twice daily) or adagrasib (at the same dose) in combination with intravenous cetuximab once a week (with an initial loading dose of 400 mg per square meter of body-surface area, followed by a dose of 250 mg per square meter) or every 2 weeks (with a dose of 500 mg per square meter). "
5.	Lung Neoplasms (Lung Cancer) 01/01/2023 - "Here, we report on early ctDNA changes of KRAS G12C in a Phase 2 trial of adagrasib in patients with advanced, KRAS G12C-mutant lung cancer. " 10/01/2022 - "Adagrasib shines in a lung cancer trial." 07/01/2023 - "Additionally, SHP2 overexpression enhanced the resistance of MRTX849 to lung cancer cells. " 07/01/2023 - "SHP2 knockdown enhanced the sensitivity of MRTX849-resistant cell lines to MRTX849 and encouraged the killing of lung cancer cells by MRTX849, as indicated by a more significant decrease in cell viability and proliferation after knockdown of SHP2 in the presence of MRTX849 compared with MRTX849 untreated, while apoptosis was more significantly enhanced. " 07/01/2023 - "Lung cancer cell lines resistant to MRTX849 were first constructed by repeated dosing over 10 months, and the parental and drug-resistant strains were evaluated for SHP2 expression at different time points (2, 4, 6, 8, 10 months). "

Related Drugs and Biologics

1.	sotorasib
2.	adagrasib
3.	pembrolizumab
4.	Cysteine (L-Cysteine)
5.	Cetuximab (Erbitux)
6.	Glycine (Aminoacetic Acid)
7.	Codon (Codons)
8.	Proteins (Proteins, Gene)
9.	ErbB Receptors (EGF Receptor)
10.	B7-H1 Antigen

Related Therapies and Procedures

1.	Therapeutics
2.	Immunotherapy
3.	Drug Therapy (Chemotherapy)
4.	Oral Administration
5.	Treatment Delay