Journal of medicinal chemistryProdrugsHumansSolubilityBiological AvailabilityAdministration
Enhancing the Oral Bioavailability of a Poorly Soluble Pan-CK2 Kinase Inhibitor: Leveraging a Phosphate Prodrug Strategy to Overcome Dissolution-Limited Absorption and Improve Systemic Exposure during Dose Escalation.
Murugaiah A M Subbaiah, Naveen Manjunath, Thangeswaran Ramar, Mathiazhagan Annadurai, Naveen Kumar Dhondi, Tarun Sharma, Sheelendra Singh, Megha Thakur, Priyadeep Bhutani, Shahe Mahammad, Srinivas Kasibhatla, Sridhar Desikan, Kurt Zimmermann, Xiaopeng Sang, Gerry Everlof
Published: 202610.1021/acs.jmedchem.5c03141
Abstract
BMS-135, a preclinical casein kinase 2 (CK2) inhibitor, demonstrated subnanomolar potency, robust cellular antiproliferative activity, and pronounced antitumor efficacy in xenograft models. However, its poor solubility posed significant challenges fo…
Preview only. Read the full abstract at the source