TheRas, Inc., operating under the name BridgeBio Oncology Therapeutics ("BBOT" or the "Company"), a biopharmaceutical firm currently in clinical development targeting RAS-pathway cancers, has reported that the initial patient has received the BBO-10203 treatment in the BREAKER-101 study. BBO-10203 represents a novel class of orally available RAS:PI3Ka breaker that prevents the interaction between RAS and PI3Kα, effectively hindering PI3Kα-AKT signaling in tumors, while not directly affecting the enzymatic function of PI3Kα.
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“I am excited to collaborate with BBOT in introducing a groundbreaking potential therapy to clinical settings,” stated Dr. Minal Barve, Chief Medical Officer and Principal Investigator at Mary Crowley Cancer Research in Dallas, TX. “BBO-10203 is a first-in-class compound with the ability to meet significant unmet medical needs, potentially altering the landscape of cancer treatment. We eagerly anticipate examining BBO-10203 in the BREAKER-101 trial.”
BBO-10203 is specifically engineered to covalently and selectively interact with the RAS-binding domain (RBD) of PI3Kα. This targeted inhibition works independently of the mutational status of PI3Kα and RAS and has shown in preclinical models complete suppression of RAS-driven pAKT signaling at low nanomolar concentrations. Furthermore, preclinical studies demonstrated that treatment with BBO-10203 did not lead to hyperglycemia in animal models. The development of BBO-10203 resulted from a partnership involving the RAS Initiative at Frederick National Laboratory, Lawrence Livermore National Laboratory, and BBOT.
“BBO-10203 represents a groundbreaking initiative that disrupts the interaction between the two most commonly mutated oncogenes found in human cancers, offering us a unique chance to evaluate the significance of RAS-coordinated activation of the MAPK and AKT pathways for the first time,” remarked Pedro Beltran, PhD, Chief Scientific Officer at BBOT. “The identification of BBO-10203 was made possible through the concerted efforts of academic institutions, national laboratories, and industry professionals collaborating to enhance therapeutic options for cancer patients.”
The BREAKER-101 trial aims to recruit participants worldwide who have locally advanced or metastatic HER2-positive breast cancer, HR-positive/HER2-negative breast cancer, KRAS mutant advanced colorectal cancer, and KRAS mutant advanced non-small cell lung cancer.
“There is significant potential to elevate the standard of oncology care by targeting oncogenic pAKT signaling while avoiding the metabolic side effects typically seen with kinase inhibitors. The launch of the Phase 1 study of BBO-10203 signifies a critical development in this area,” commented Yong (Ben) Ben, MD, Chief Medical and Development Officer at BBOT. “Submitting a second IND within just six months after forming BBOT highlights our team’s ability to advance innovative programs to clinical application. This unique mechanism and the scientific foundation supporting it will create exciting combination strategies that effectively inhibit both pAKT and pERK, which we hope will provide exceptional benefits to patients with RAS-driven tumors.”
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According to the data provided by the Synapse Database, As of October 31, 2024, there are 102 investigational drugs for the PI3Kα target, including 230 indication, 128 R&D institutions involved, with related clinical trial reaching 466, and as many as 6144 patents.
The drug BBO-10203 is a small molecule drug that targets PI3Kα. It is being developed for the treatment of various therapeutic areas, including neoplasms, digestive system disorders, respiratory diseases, and skin and musculoskeletal diseases. The active indications for BBO-10203 include advanced breast cancer, advanced HER2-Positive breast carcinoma, advanced malignant solid neoplasm, HER2 positive cancer, KRAS mutant colorectal cancer, metastatic breast cancer, metastatic colorectal carcinoma, and metastatic lung cancer.