Towards streamlined product information: reporting of transporter-mediated drug interactions.

Purpose: The purpose of this study is to investigate the reporting of risks associated with transporter-mediated drug-drug interactions (DDIs) in medicinal product information and to identify suitable wording for future standardisation of summaries of product characteristics (SmPCs).

Methods: The SmPCs of medicinal products approved in the European Union from 2012 to 2023 were screened for warnings on Organic Anion Transporting Polypeptide 1B1 and 1B3 (OATP1B1 and OATP1B3), and Breast Cancer Resistance Protein (BCRP). An in-house search engine for product information was used.

Synthesis, Microtubule-Binding Affinity, and Antiproliferative Activity of New Epothilone Analogs and of an EGFR-Targeted Epothilone-Peptide Conjugate.

A new simplified, epoxide-free epothilone analog was prepared incorporating an N-(2-hydroxyethyl)-benzimidazole side chain, which binds to microtubules with high affinity and inhibits cancer cell growth in vitro with nM potency. Building on this scaffold, a disulfide-linked conjugate with the purported EGFR-binding (EGFR, epidermal growth factor receptor) peptide GE11 was then prepared. The conjugate retained significant microtubule-binding affinity, in spite of the size of the peptide attached to the benzimidazole side chain.