Clinical management of metastatic colorectal cancer in the era of precision medicine

F Ciardiello, D Ciardiello, G Martini… - CA: a cancer journal …, 2022 - Wiley Online Library
Colorectal cancer (CRC) represents approximately 10% of all cancers and is the second
most common cause of cancer deaths. Initial clinical presentation as metastatic CRC …

Rational combinations of targeted cancer therapies: background, advances and challenges

H Jin, L Wang, R Bernards - Nature Reviews Drug Discovery, 2023 - nature.com
Over the past two decades, elucidation of the genetic defects that underlie cancer has
resulted in a plethora of novel targeted cancer drugs. Although these agents can initially be …

[HTML][HTML] Sotorasib plus Panitumumab in Refractory Colorectal Cancer with Mutated KRAS G12C

MG Fakih, L Salvatore, T Esaki… - … England Journal of …, 2023 - Mass Medical Soc
Abstract Background KRAS G12C is a mutation that occurs in approximately 3 to 4% of
patients with metastatic colorectal cancer. Monotherapy with KRAS G12C inhibitors has …

[HTML][HTML] Single-Agent Divarasib (GDC-6036) in Solid Tumors with a KRAS G12C Mutation

A Sacher, P LoRusso, MR Patel… - … England Journal of …, 2023 - Mass Medical Soc
Abstract Background Divarasib (GDC-6036) is a covalent KRAS G12C inhibitor that was
designed to have high potency and selectivity. Methods In a phase 1 study, we evaluated …

[HTML][HTML] Sotorasib in KRAS p.G12C–Mutated Advanced Pancreatic Cancer

JH Strickler, H Satake, TJ George… - New England journal …, 2023 - Mass Medical Soc
Abstract Background KRAS p. G12C mutation occurs in approximately 1 to 2% of pancreatic
cancers. The safety and efficacy of sotorasib, a KRAS G12C inhibitor, in previously treated …

[HTML][HTML] Adagrasib with or without Cetuximab in Colorectal Cancer with Mutated KRAS G12C

R Yaeger, J Weiss, MS Pelster, AI Spira… - … England Journal of …, 2023 - Mass Medical Soc
Background Adagrasib, an oral small-molecule inhibitor of mutant KRAS G12C protein, has
shown clinical activity in pretreated patients with several tumor types, including colorectal …

The current state of the art and future trends in RAS-targeted cancer therapies

SR Punekar, V Velcheti, BG Neel… - Nature reviews Clinical …, 2022 - nature.com
Despite being the most frequently altered oncogenic protein in solid tumours, KRAS has
historically been considered 'undruggable'owing to a lack of pharmacologically targetable …

Adagrasib in Advanced Solid Tumors Harboring a KRASG12C Mutation

TS Bekaii-Saab, R Yaeger, AI Spira… - Journal of Clinical …, 2023 - ascopubs.org
PURPOSE Adagrasib, a KRASG12C inhibitor, has demonstrated clinical activity in patients
with KRAS G12C-mutated non–small-cell lung cancer (NSCLC) and colorectal cancer …

The ascension of targeted covalent inhibitors

J Singh - Journal of Medicinal Chemistry, 2022 - ACS Publications
Covalent drugs have made a major impact on human health but until recently were shunned
by the pharmaceutical industry over concerns about the potential for toxicity. A resurgence …

Drugging KRAS: current perspectives and state-of-art review

K Parikh, G Banna, SV Liu, A Friedlaender… - Journal of hematology & …, 2022 - Springer
After decades of efforts, we have recently made progress into targeting KRAS mutations in
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …