Hope Biosciences Acquires Worldwide Rights To Novel MERTK/AXL Inhibitor From NeoPharm

By: PRLog
- High potency (at nanomolar concentration) against MERTK, a promising I-O target;
- Overcomes AXL/c-MET mediated resistance to EGFR-directed therapies in NSCLC in vivo;
- Ready for IND submission in 2018

IRVINE, Calif. - Feb. 1, 2017 - PRLog -- HOPE BIOSCIENCES, INC. announced today that it has acquired exclusive and worldwide rights to develop and commercialize HOPE 777, a unique MERTK/AXL/pan-c-MET tyrosine kinase inhibitor through a licensing agreement with NeoPharm Co. Ltd, a South Korean pharmaceutical company.

HOPE 777 has undergone extensive preclinical evaluation, and the data suggest that it has an impressive potency against the receptor tyrosine kinases MERTK, AXL, and pan-c-MET, key targets of tumor growth, chemotherapy resistance, epithelial-mesenchymal transition (EMT) behind cancer metastases, and tumor immune suppression.

In-vivo studies in erlotinib (TARCEVA®)- and gefitinib (IRESSA®)-resistant non-small cell lung cancer (NSCLC) demonstrated that HOPE 777 efficiently blocked c-MET and AXL functions, the primary as well as secondary by-pass signaling pathways induced by EGFR inhibitors such as erlotinib or gefitinib. Treatment with HOPE 777 also resulted in dose-dependent reduction of tumor size and angiogenesis in glioblastoma and stomach cancer models in mice. HOPE 777 appears to have inhibited c-MET mutants that are often resistant against other c-MET inhibitors currently in development. Kinase panel profiling demonstrated specificity and potency of HOPE 777. The preliminary PK profile also indicates favorable oral bioavailability, plasma concentration, and half-life.

"We believe HOPE 777 will have multiple therapeutic applications in overcoming resistance against EGFR-directed therapies," said George Uy, CEO and founder of HOPE BIOSCIENCES. "We are also excited by HOPE 777's possible immune oncology (I-O) potential due to its high potency against MERTK, a validated I-O target. MERTK is over-expressed in tumor cells as well as tumor-associated macrophages (TAM) suppressing anti-tumor immunity. We will evaluate its I-O applications in combination with checkpoint inhibitors. Meanwhile, we will initiate IND-enabling studies and CMC scale-up. The goal is to file the IND application in the next 12-18 months and get into the clinic in 2018."

"We are excited to partner with HOPE BIOSCIENCES to develop and bring to market our RTK inhibitor program," said Yoon Kim, CTO of NeoPharm. "We are fully committed to supporting the program to address the unmet needs of patients living with cancer worldwide."


HOPE is a privately-owned biopharmaceutical company based in Irvine, California focused on licensing and commercializing anti-cancer drugs that address high unmet medical needs. HOPE has two unique assets currently in IND-enabling studies, including nuc-gemcitabine (HOPE 888), and a highly potent MERTK/AXL/pan-c-MET kinase inhibitor (HOPE 777).

"Hope in the face of difficulty. Hope in the face of uncertainty. The audacity of hope!" President Barack Obama.


NeoPharm is the leading skin care company in South Korea. NeoPharm is dedicated to bringing the best in class skin care products through innovative in-house R&D. Since its formation in 2000, NeoPharm has successfully developed and introduced several dermatological products including the No. 1 skin care for sensitive skin in South Korea.




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