CXCR4 heteromers as novel cancer targets

Dr. GPCR Summit 2021

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CXCR4 heteromers as novel cancer targets


Monday, 09/13/ 2021 @ 1:00 PM - EST
  
- Dr. Juan Jose Fung & Dr. Pina Cardarelli -
- GPCR Therapeutics USA, Inc.-
- Seoul, KOREA-

     
  

Abstract

   

CXCR4 antagonists have been pursued as antineoplastic agents with many programs advancing into clinical trials. Nevertheless, there has been limited success, with only one molecule to date gaining FDA approval in 2008. Our research demonstrates that CXCR4 has a propensity to form heteromers with other GPCRs, inducing novel pharmacology that is not fully suppressed by CXCR4 inhibition alone. Instead, antagonism of both CXCR4 and its GPCR partner is required for full efficacy. In this presentation, we introduce our lead program targeting CXCR4-B2AR heteromers in oncology and focus on the clinical direction of our lead asset Burixafor, a potent small-molecule antagonist of CXCR4 and its application in hematopoietic stem cell transplantation in multiple myeloma.

   
   

About Dr. Juan José Fung

   

Dr. Juan José Fung is a Principal Scientist at GPCR Therapeutics, Inc, a drug discovery company focused on targeting GPCR heteromers in cancer, headquartered in Seoul, Korea, with an R&D facility in the SF Bay Area. Dr. Fung received his Ph.D. from the Stanford University School of Medicine under the mentorship of Dr. Brian Kobilka, studying the dimerization of GPCRs. Dr. Fung continued his Postdoctoral training in Dr. Kobilka’s lab contributing to the elucidation of high-resolution structures of various GPCRs. Dr. Fung has spent significant time in the industry studying membrane proteins, antibodies, and HTS methods for drug discovery. His current work is mainly focused on screening and assay development to bridge the gap between in vitro and in vivo GPCR pharmacology.
    

   

Dr. Juan José Fung on the web

        
     

About Dr. Josephine (Pina) Cardarelli

   
Dr. Pina Cardarelli, CSO for GPCR Therapeutics Inc., based in South Korea, has recently been named President of GPCR Therapeutics, USA, a newly incorporated Biotechnology company in the Bay Area. The company’s mission is to discover and develop highly effective cancer therapeutics by targeting heteromers of G protein-coupled receptors (GPCR). Burixafor, their most advanced clinical candidate, will be in Phase II clinical trial next year. Additionally, they have a library of target GPCR heteromers for Oncology. Dr. Cardarelli heads the team of talented researchers that will be expanding at the US site.

Dr. Cardarelli is a drug development leader with extensive experience driving drug discovery teams in bringing biologics to clinical proof of concepts. She has expertise in cell biology, pharmacology, translational medicine, oncology, immuno-oncology, immunology, and clinical development. Previously, she held the position of Vice President of Cell Biology & Pharmacology, at Bristol-Myers Squibb. She was an integral contributor to two therapeutics that are FDA approved, Yervoy and Opdivo. She was a participant in numerous due diligence (anti-CXCL8 mAb) and has managed external collaborations and alliances. Prior to this, she held the position of Vice President, at Medarex, Inc. While at BMS and Medarex, she led programs from target ID to clinical development that included, CXCL10 (Eldelumab), CXCR4 (Ulocuplumab), CD30, CD19, Fucosyl GM-1, & mesothelin-ADC, Glypican-3-ADC, CD70-ADC. She oversaw early discovery programs IL-23 p19 and IL23 p19/IL-17 bispecifics. At Medarex, she initiated and identified the lead mAb for the type I interferon-alpha receptor project, licensed to AstraZeneca (Saphnelo™ Anifrolumab) that has just received FDA approval for systemic lupus erythematosus. She has extensive experience working with Biologics, and Antibody Drug Conjugates as well as experience in IND fillings, IB updates, and responding to FDA inquiries. She is an inventor on 39 issued U.S. patents including anti-PD-1 patents, 22 EP patents, and greater than 100 global patents centered around therapeutic development. She has also authored forty-six peer-reviewed publications. Dr. Cardarelli received her Ph.D. in Physiology from Albany Medical College.
 

Dr. Josephine (Pina) Cardarelli on the web

       
 

Author list and affiliations

  
  • Juan José Fung, Ph.D. and Pina Cardarelli, Ph.D., GPCR Therapeutics, USA

   

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