ITX-5061 / iTherX - LARVOL DELTA

Inhibitors Targeting Hepatitis C Virus (HCV) Entry. (PubMed, Mini Rev Med Chem) - "Among the inhibitors found in the literature, ITX 5061 corresponds to the most effective one, with EC and CC values of 0.25 nM and >10 μM (SI: 10,000), respectively...Interestingly, chlorcyclizine (an antihistamine drug) showed action both in E1 apolipoproteins (EC and CC values of 0.0331 and 25.1 μM, respectively), as well as in NPC1L1 (IC and CC values of 2.3 nM and > 15 μM, respectively). Thus, this review will discuss promising inhibitors targeting HCV entry, discussing their SAR analyzes, recent contributions, and advances in this field."

Journal • Fibrosis • Gastrointestinal Cancer • Hepatitis C • Hepatocellular Cancer • Hepatology • Immunology • Infectious Disease • Inflammation • Oncology • Solid Tumor

Deciphering the role of cholesterol in the radiation response of glioblastoma (ESTRO 2023) - "Treatment for glioblastoma comprises surgery, radiation, and chemotherapy with temozolomide...These included ITX-5061 (cholesterol uptake); the statins pitavastatin, simvastatin, fluvastatin, lovastatin, and AY9944 (cholesterol synthesis); LXR-623 (transcriptional control of cholesterol genes); evodiamine (cholesterol efflux); avasimibe, rubamaillin, and efavirenz (cholesterol esterification); and U18666A (intracellular cholesterol transport and trafficking)...A better understanding of cholesterol homeostasis in cancer cells is needed to identify appropriate combinations and schedules, resulting in consistent clinical responses and ultimately improving patient outcomes. These preliminary findings place cholesterol trafficking as an alternative cancer-specific pathway for targeting cholesterol in glioblastoma, offering an exciting, novel therapeutic avenue for cancer treatment, warranting further investigation."

Brain Cancer • CNS Tumor • Gastrointestinal Cancer • Glioblastoma • Hepatology • Oncology • Pancreatic Cancer • Solid Tumor • NPC2 • STARD3NL

Evaluating the Safety of ITX 5061 in Treatment-Naive Hepatitis C (HCV)-Infected Adults (clinicaltrials.gov) - P1b; N=30; Completed; Sponsor: National Institute of Allergy and Infectious Diseases (NIAID); Phase classification: P1 ➔ P1b

Clinical • Phase classification • Hepatitis C • Hepatology • Infectious Disease • Inflammation

[VIRTUAL] Exploiting Cholesterol Metabolism to Treat Primary and Metastatic Renal Carcinoma (KCRS 2021) - "Moreover, pharmacological inhibition of SCARB1 using a novel compound (ITX-5061) results in decreased ccRCC cell proliferation in vitro...The impact of this KCRP Idea Development Application comes from the pressing need for new therapeutic strategies, given that targeted therapies, anti-angiogenics, immunotherapies, and other metabolic strategies (such as targeting glutamine metabolism) only serve subsets of patients, even in combination, and altered cholesterol metabolism is a universal feature of ccRCC. Finally, as HIF-2alpha antagonists continue to be tested in ongoing clinical trials, SCARB1 inhibition could be deployed in patients ultimately acquiring resistance to HIF-2alpha-specific drugs, as previously demonstrated in preclinical studies."

IO biomarker • Clear Cell Renal Cell Carcinoma • Genito-urinary Cancer • Hepatology • Inflammation • Kidney Cancer • Oncology • Renal Cell Carcinoma • Solid Tumor • EPAS1

MEAN inhibits hepatitis C virus replication by interfering with a polypyrimidine tract-binding protein. (PubMed) - "Drug combination usage analyses demonstrated that MEAN was synergistic with interferon α, ITX5061 and ribavirin. In the host cytoplasm, PTB is directly associated with HCV replication, and the inhibition of HCV replication by MEAN can result in the sequestration of PTB in treated nuclei. Taken together, these results indicate that MEAN is a potential therapeutic candidate for HCV infection, and the targeting of the nucleo-cytoplasmic translocation of the host PTB protein could be a novel strategy to interrupt HCV replication."

Journal • Biosimilar • Hepatitis C Virus • Immunology • Infectious Disease