ronacaleret (GSK751689) / GSK - LARVOL DELTA

Significance of gut breast cancer resistance protein versus organic anion transporting polypeptide 2B1 inhibition on rosuvastatin clinical drug-drug interactions. (PubMed, Drug Metab Dispos) - "Organic anion transporting polypeptide (OATP)2B1 facilitates oral absorption of many drugs including celiprolol, fexofenadine, and rosuvastatin. Strong BCRP inhibition, with a G-value >100, translated to "positive" DDIs, whereas "OATP2B1-alone" inhibitors may lead to "negative" DDIs. For example, ronacaleret and elagolix significantly reduced rosuvastatin area under the curve due to strong OATP2B1 inhibition but weak BCRP inhibition."

Journal • Breast Cancer • Oncology • Solid Tumor • SLCO2B1

Development of a more sustainable process for ronacaleret hydrochloride (ACS-Fall 2022) - "By addressing the major environmental and economic disadvantages of the earlier route, a much more sustainable and robust process for the manufacturing of SB-751689-A had been developed which enable the production of metric tons of SB-751689-A for clinical studies. This talk will describe the process development for the new route and its major improvements over the previous route."

Musculoskeletal Diseases • Orthopedics • Osteoporosis • Rheumatology

To Estimate Relative Bioavailability of 5 Formulations of Ronacaleret Given to Healthy Postmenopausal Females (clinicaltrials.gov) - P1; N=32; Completed; Sponsor: GlaxoSmithKline; Phase classification: P=N/A ➔ P1

Phase classification • Biosimilar

A Phase IIa Study Of Men And Post-Menopausal Women With A Fractured Distal Radius (clinicaltrials.gov) - P2a; N=86; Terminated; Sponsor: GlaxoSmithKline; Trial primary completion date: Nov 2012 ➔ Nov 2008

Trial primary completion date • Biosimilar

Anti-albuminuric actions of calcilytics in the remnant kidney. (PubMed) - "The present data indicate that ronacaleret preserves klotho expression and renal function with reductions in serum phosphate and albuminuria in 5/6-nephrectomized rats. Our findings demonstrate that vitamin D prevents declines in klotho expression and renal function, suppressing albuminuria."

Journal • Biosimilar • Chronic Kidney Disease • Renal Disease

Klotho Protein Supplementation Retards Renal Injury in 5/6-Nephrectomized Rats (KIDNEY WEEK 2019) - "Background We have previously reported that ronacaleret, a calcilytic agent, retards renal injury by increasing endogenous klotho expression in remnant kidney model (Am J Physiol Renal Physiol...in remnant kidney. Funding Government Support - Non-U.S."

Preclinical