P-Glycoprotein (ABCB1/MDR1) and BCRP (ABCG2) Limit Brain Accumulation and Cytochrome P450-3A (CYP3A) Restricts Oral Exposure of the RET Inhibitor Selpercatinib (RETEVMO) - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/34832869/
1 Division of Pharmacology, The Netherlands Cancer Institute, Plesmanlaan 121, 1066 CX Amsterdam, The Netherlands. 2 Department of Pharmaceutical Sciences, Division of Pharmacology, Faculty of Science, Utrecht University, Universiteitsweg 99,...
Conclusion/Relevance: CYP3A-mediated metabolism can limit selpercatinib oral exposure and hence its tissue concentrations. These insights may be useful in the further clinical development of selpercatinib.
Untangling the KRAS mutated lung cancer subsets and its therapeutic implications - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/34918209/
The Kirsten rat sarcoma virus transforming protein (KRAS) mutations (predominate in codons 12, 13, and 61) and genomically drive nearly one-third of lung carcinomas. These mutations have complex functions in...
Conclusion/Relevance: We summarize the existing knowledge of KRAS mutations and their coexisting mutations that is relevant to lung cancer treatment, in this review. We elaborate on the prognostic impact of clinical and pathologic characteristics of lung cancer patients associated with KRAS mutations. We briefly review the currently available...
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NSCLC Connect4yrKey Points • Source: Molecular Biomedicine • Relevance: “We briefly review the currently available techniques for KRAS mutation detection on biopsy and cytology samples. Finally, we discuss the new therapeutic strategies for targeting KRAS-mutant Show More
Safety and effectiveness of ramucirumab and docetaxel: a single-arm, prospective, multicenter, non-interventional, observational, post-marketing safety study of NSCLC in Japan
Source : https://www.tandfonline.com/doi/abs/10.1080/14740338.2022.2023127?journalCode=ieds20
Abstract This study evaluated the safety and effectiveness of ramucirumab plus docetaxel treatment for non-small cell lung cancer (NSCLC) in the real-world setting. This single-arm, prospective, multicenter, non-interventional, post-marketing study...
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Conclusions: Data from real-world settings demonstrates that ramucirumab plus docetaxel treatment appears to be tolerable and effective in Japanese patients regardless of patient baseline characteristics and prior treatment.
Multicenter real‐world data of patients harboring rare mutations other than EGFR or ALK in advanced or metastatic non‐small cell lung cancer
Source : https://onlinelibrary.wiley.com/doi/10.1111/1759-7714.14266
Chang Min Choi , Corresponding Author Chang Min Choi Department of Pulmonary and Critical Care Medicine, Asan Medical Center, University of Ulsan College of Medicine, Seoul, South Korea Department of...
Conclusions: First-line platinum-based chemotherapy showed durable benefit in patients with advanced or metastatic nonsquamous NSCLC harboring rare genetic mutation other than EGFR or ALK.
![Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3- d]pyrimidine RET Inhibitors - PubMed](https://static-content-prd.skipta.com/public/skipta/skipta-post/2023-02/pubmed-meta-image_1188.png "Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3- d]pyrimidine RET Inhibitors - PubMed")
Antitarget Selectivity and Tolerability of Novel Pyrrolo[2,3- d]pyrimidine RET Inhibitors - PubMed
Source : https://pubmed.ncbi.nlm.nih.gov/34917254/
The selective inhibition of RET kinase as a treatment for relevant cancer types including lung adenocarcinoma has garnered considerable interest in recent years and prompted a variety of efforts toward...
Conclusion: The optimization of this pyrrolo[2,3-d]pyrimidine core resulted in compound 1, which demonstrated potent in vitro RET kinase inhibition and robust in vivo efficacy in RET-driven tumor xenografts upon multiday dosing in mice. The administration of 1 was well-tolerated at established efficacious doses (10 and 30 mg/kg, po, qd), and...