litronesib (KF 89617) / Kyowa Kirin, Eli Lilly - LARVOL DELTA

ABCB1 overexpression confers resistance to litronesib, an Eg5 inhibitor. (PubMed, Biochem Pharmacol) - "ABCB1 overexpression conferred robust resistance to litronesib, which was reversed by verapamil. Litronesib induced a higher fold resistance than the classical ABCB1 substrates paclitaxel and doxorubicin (P < 0.05), and failed to reverse ABCB1-mediated multidrug resistance at non-cytotoxic concentrations...Litronesib exhibits pronounced ABCB1-mediated resistance, a finding that underscores the need for strategies such as patient stratification or structural optimization to enhance efficacy. These findings provide a crucial framework for the resistance-aware development of new Eg5 inhibitors and will inform their future clinical applications."

Journal • Oncology • ABCB1 • ABCC1 • ABCG2 • KIF11

KIF11 as a druggable target in NSCLC: An integrated computational analysis. (ASCO 2026) - "DGIdb analysis prioritized KIF11 as the most actionable hub, led by ispinesib–KIF11 and filanesib, followed by litronesib, AZD-4877, dimethylenastron, S-Trityl-L-cystein (STLC). This study highlights STLC as a promising KIF11 inhibitor with strong structural engagement and favorable in silico developability, alongside ispinesib as a validated reference, supporting KIF11 as a central, druggable vulnerability in female non-smoking NSCLC with potential relevance across broader NSCLC subgroups. In silico binding, ADMET, and OSIRIS drug-likeness profiles of KIF11 inhibitors. Abbreviations: HIA, human intestinal absorption; AMES, Ames mutagenicity test; hERG, human ether-a-go-go–related gene channel."

Lung Cancer • Non Small Cell Lung Cancer • Solid Tumor • BUB1 • CCNA2 • CCNB1 • CDK1 • KIF11 • MELK • TOP2A

Kinesin spindle protein inhibitors in cancer: from high throughput screening to novel therapeutic strategies. (PubMed, Future Sci OA) - "In this review, we track the medicinal chemistry developmental stages of KSP inhibitors. Moreover, we address the challenges that are faced during the development of KSP inhibitor therapy for cancer and future insights for the latest advances in research that are directed to find active KSP inhibitor drugs."

Journal • Review • Oncology

Role of KSP inhibitors as anti-cancer therapeutics: an update. (PubMed, Anticancer Agents Med Chem) - "Drugs such as filanesib, litronesib, ispinesib have entered clinical trials, the most advanced phase explored being Phase II. KSP inhibitors have exhibited promising results; however, continued exploration is greatly required to establish the clinical potential of KSP inhibitors."

Journal • Allergy • Oncology • Pain

Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing. (PubMed, Viruses) - "To that end, using three bacteria-based assays, we screened a library of 2839 approved-for-human-use drugs and identified the following potential channel-blockers: Capreomycin, Pentamidine, Spectinomycin, Kasugamycin, Plerixafor, Flumatinib, Litronesib, Darapladib, Floxuridine and Fludarabine. The stage is now set for examining the activity of these compounds in detailed electrophysiological studies and their impact on the whole virus with appropriate biosafety measures."

Journal • Infectious Disease • Novel Coronavirus Disease • Respiratory Diseases

A Study in Ovarian, Non-Small Cell Lung, Prostate, Colorectal, Gastroesophageal Cancers, and Squamous Cell Carcinoma of the Head and Neck (clinicaltrials.gov) - P2; N=103; Completed; Sponsor: Eli Lilly and Company; N=250 ➔ 103

Clinical • Enrollment change

A Study in Ovarian, Non-Small Cell Lung, Prostate, Colorectal, Gastroesophageal Cancers, and Squamous Cell Carcinoma of the Head and Neck (clinicaltrials.gov) - P2; N=250; Completed; Sponsor: Eli Lilly and Company; Active, not recruiting ➔ Completed

Clinical • Trial completion