.Pharmacolibrary.Drugs.L_AntineoplasticAndImmunomodulatingAgents.L01E_ProteinKinaseInhibitors.L01EB05_Rociletinib.Rociletinib

Information

Rociletinib is an oral, small molecule, irreversible inhibitor of mutant forms of the epidermal growth factor receptor (EGFR), developed for the treatment of non-small cell lung cancer (NSCLC) with EGFR T790M mutation. It showed clinical promise in early trials but has since been discontinued and is not approved for clinical use.

Pharmacokinetics

Pharmacokinetic parameters in adult patients with advanced non-small cell lung cancer (NSCLC), as reported in phase I/II clinical studies.

References

1. Ballard, P, et al., & Cross, D (2016). Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity. Clinical cancer research : an official journal of the American Association for Cancer Research 22(20) 5130–5140. DOI:10.1158/1078-0432.CCR-16-0399 PUBMED:https://pubmed.ncbi.nlm.nih.gov/27435396

Revisions

• 06/2025 initial generated model