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GPCR Therapeutics Announces Publication in Nature Scientific Reports on Novel Anticancer Therapy
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- CXCR4-HRH1 heteromer identified as a potential therapeutic target for anticancer therapy
Seoul, Korea, & Redwood City, California, 15 March 2023 – GPCR Therapeutics, Inc., a clinical stage, international biopharmaceutical company focused on targeting G Protein Coupled Receptors (GPCR) pairs, announced publication of a paper in Nature Scientific Reports (1), in collaboration with the School of Biological Sciences, Seoul National University (Seoul, Republic of Korea). The paper is entitled ‘Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration.’
CXC chemokine receptor 4 (CXCR4) is a well-known GPCR overexpressed in more than 23 types of cancer and plays an important role in tumor metastasis. The team, led by Professor Won-Ki Huh, shows that another GPCR known as histamine receptor H1 (HRH1) is widely expressed in various cancer cell lines and cancer tissues, and that the level of co-expression of CXCR4 and HRH1 is related to poor prognosis in breast cancer patients. The simultaneous expression of both receptors leads to the formation of CXCR4-HRH1 heteromer, and this complex demonstrates enhanced signalling and migration capabilities.
These findings suggest the interaction of CXCR4 and HRH1 may play an important role in cancer progression, thus serving as a potential therapeutic target for anticancer therapy.
Dr. Michel Bouvier, a world-renowned expert in the field of GPCRs working as a professor and CEO at the Institute for Research in Immunology and Cancer (IRIC) at Université de Montréal said, “This paper shows that the co-expression of the CXCR4 chemokine receptor and the H1 histamine receptor is associated to a poor prognostic and shorter overall and progression-free survival in breast cancer patients. This synergism between CXCR4 and HRH1 was observed not only in breast cancer cells but also in other cancer cells in which both receptors are expressed, suggesting a possible generalization of this cross-talk mechanism in oncogenesis. The observation that CXCR4 and HRH1 can form heterodimers in live cells suggest that such heterodimerization may underlie the observed synergism between the two receptors and open the possibility of targeting such heterodimer for the development of anti-cancer drugs.”
“We are on a scientific journey to find more efficacious cancer treatments, delivering better patient outcomes,” commented Dr. Dong Seung Seen, GPCR’s founder and CEO. “We believe understanding the interactions between GPCRs is the key to overcoming the current hurdles of drug discovery. This publication is significant as it represents the first case for our co-targeting drug development strategy to be peer-reviewed and validated in academia. In addition to the ongoing combination treatment program using a CXCR4 inhibitor, GPC-100, and an ADRB2 inhibitor, Propranolol, we plan to expand our pipeline by targeting the interaction of CXCR4 and other GPCRs in the development of anticancer drugs.”
GPCR recently announced the launch of a US phase 2 trial of GPC-100 in combination with Propranolol for stem cell mobilization in patients with multiple myeloma (2).
References
(1) Simultaneous activation of CXC chemokine receptor 4 and histamine receptor H1 enhances calcium signaling and cancer cell migration:
https://www.nature.com/articles/s41598-023-28531-1
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Media contacts:
GPCR Therapeutics (in Seoul)
DaYoon Kim – Business Development Manager
Tel: +82-2-878-2848
Scius Communications (in London)
Katja Stout
Tel: +44 778 943 5990
Daniel Gooch
Tel: +44 774 787 5479
daniel@sciuscommunications.com
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.
GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for multiple solid tumors as well as hematological malignancies. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, and has demonstrated safety and efficacy in US Phase 2 clinical trial. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation. This combination therapy is currently undergoing Phase 2 clinical trial in the US. The company is collaborating with Australia’s AdAlta on novel cancer therapeutics.
GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn
GPCR Therapeutics Announces Launch of US Phase 2 Trial of GPC-100 in Multiple Myeloma
- The trial will evaluate the safety and efficacy of GPCR’s CXCR4-targeting stem cell mobilizer, GPC-100, in combination with propranolol
- The trial will also evaluate the potential of the combined treatment to replace G-CSF
Seoul, Korea, & Redwood City, California, 17 January 2023 – GPCR Therapeutics, Inc., a venture-backed, clinical stage, international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, announced today the initiation of their phase 2 trial in the US for its lead small molecule asset, GPC-100. GPC-100 targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in more than 23 cancers.
This randomized, open-label phase 2 study assesses the efficacy of GPC-100 and propranolol, with and without granulocyte colony-stimulating factor (G-CSF) for the mobilization of stem cells in patients with multiple myeloma undergoing autologous stem cell transplant. Propranolol blocks beta adrenergic receptors, also part of the GPCR family of proteins. G-CSF is a glycoprotein that stimulates the bone marrow to produce granulocytes and stem cells and release them into the bloodstream. The trial is for up to 40 adult patients who will be enrolled at cancer centers in the USA. The trial will include a total of ten clinical sites, with University of Massachusetts Chan Medical School selected as the first clinical site to be activated. Muthalagu Ramanathan, M.D. will serve as the Principal Investigator. Trial completion is expected to be in the summer of 2024.
Dr. Dong Seung Seen, GPCR’s founder and CEO, said, “The initiation of this Phase 2 trial is the result of lengthy and meticulous work by our teams in California and Seoul. I thank them for their unwavering dedication and determination to make a difference to people with cancer.”
Dr. Omar Nadeem, Clinical Director for Myeloma Cellular Therapies Program at the Dana-Farber Cancer Institute, and a member of GPCR’s Scientific Advisory Board, commented, “This trial is studying novel strategies for stem cell collection in multiple myeloma, including a non-G-CSF approach and evaluating the role of propranolol in enhancing stem cell collection yield. This would allow for improved patient experience by making the process more efficient while limiting the toxicity of the currently utilized methods.”
Dr. Pina Cardarelli, GPCR’s CSO and President of U.S. operations, said, “This is a major milestone on our scientific journey to discover specific combinations of drugs that are more efficacious for cancer treatment, delivering better patient outcomes.”
Multiple myeloma is a cancer that forms in a type of white blood cell called a plasma cell, which, when healthy, help fight infections by making antibodies that recognize and attack germs. In multiple myeloma, cancerous plasma cells accumulate in the bone marrow and crowd out healthy blood cells, no longer producing helpful antibodies, but abnormal proteins that can cause complications, such as bone pain and kidney abnormalities. In 2019, over 32,000 patients in the US were diagnosed with this disease, with a median age of 68 years at diagnosis. (1)
Reference
(1) https://rarediseases.org/rare-diseases/multiple-myeloma/
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Media contacts:
GPCR Therapeutics (in Seoul)
DaYoon Kim – Business Development Manager
Tel: +82-2-878-2848
Scius Communications (in London)
Katja Stout
Tel: +447789435990
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.
GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for multiple solid tumors as well as hematological malignancies. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation. The company is collaborating with Australia’s AdAlta (ASX: 1AD) on novel cancer therapeutics.
GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn.
ADALTA AND GPCR THERAPEUTICS COLLABORATE ON NOVEL CANCER THERAPEUTICS
- AdAlta and GPCR Therapeutics form collaboration to evaluate a new cancer treatment approach combining beta blockers plus AdAlta’s CXCR4-inhibiting i-bodies.
- CXCR4 is overexpressed in more than 23 cancers and drugs targeting the CXCR4 pathway address a multi-billion dollar opportunity.
- AdAlta has the first option to license and further commercialise any products resulting from the collaboration.
MELBOURNE Australia and SEOUL South Korea, 13 October 2022: AdAlta Limited (ASX:1AD), the clinical stage drug discovery company developing novel therapeutic products from its i-body platform and GPCR Therapeutics Inc, a clinical stage biotech company discovering and developing innovative therapeutics targeting cancer based on the novel science of CXCR4, announce a collaboration to evaluate AdAlta’s CXCR4 inhibiting i‑bodies as cancer therapeutics, using GPCR Therapeutics’ proprietary combination inhibition approach.
AdAlta’s i-body platform is ideally suited to engaging an important class of drug targets called G-protein coupled receptors (GPCRs). One of these GPCRs is known as CXCR4. In addition to its role in fibrotic disease, CXCR4 is also known to be over-expressed in more than 23 cancers, representing a multi-billion dollar drug market. Attempts by others to develop CXCR4 inhibitors as cancer therapeutics have had limited success to date.
AdAlta owns a panel of i-bodies which inhibit CXCR4 signalling in different ways. The panel includes AD-214, AdAlta’s lead drug candidate which has been progressed to clinical development for fibrotic diseases.
GPCR Therapeutics has discovered that combining CXCR4 inhibitors with molecules inhibiting other GPCRs that are associated with CXCR4 in cancer can result in superior inhibition of CXCR4.
AdAlta’s CEO and Managing Director, Tim Oldham, commented:
“We are delighted to announce this collaboration with GPCR Therapeutics. Through the program, we hope to demonstrate that AdAlta’s i-bodies, when combined with other GPCR inhibitors can have enhanced therapeutic outcomes in cancer, in comparison with the typical approach of inhibiting individual GPCRs. This collaboration is consistent with our strategy of expanding the commercial use of our i-bodies in a cost-effective way.”
GPCR Therapeutics’ CEO, Dong Seung Seen, commented:
“We are pleased to be working with AdAlta’s expert team to explore synergies between our approach for combination inhibition of GPCRs and AdAlta’s i-body technology. We believe combining AdAlta’s unique i-body technology with our innovative CXCR4 combination therapy-based approach could lead to best-in-class anticancer drugs.”
Under the collaboration, AdAlta will supply a panel of its CXCR4 inhibiting i-bodies. GPCR Therapeutics will evaluate those i-bodies in combination with a series of generic beta blocker molecules selected from its own platforms which inhibit a GPCR known as B2AR. These studies will evaluate the effect of the combined CXCR4-B2AR inhibition on in vitro cell signalling, cell migration and cell killing. If successful, GPCR Therapeutics will evaluate the combined inhibition of these compounds in vivo in mouse cancer models.
If those studies are successful, AdAlta will have the first option to license and further commercialise resulting products for treating cancer, while GPCR Therapeutics will have the same option if it is not exercised by AdAlta. The parties have agreed that whichever is the licensee under these options will pay the other pre-agreed up-front option exercise fees, development milestones, commercialisation milestones and low- to mid- single digit royalties on sales, subject to development success.
The supply of the initial panel of i-bodies under the collaboration agreement will not have a material impact on AdAlta’s cash runway or other programs.
GPCR Therapeutics were advised by Liberi Group’s CEO, Frans Trouwen.
Authorised for lodgement by:
Tim Oldham
CEO and Managing Director
September 2022
Notes to Editors
About AdAlta
AdAlta Limited is a clinical stage drug development company headquartered in Melbourne, Australia. The Company is using its proprietary i-body technology platform to solve challenging drug targeting problems and generate a promising new class of single domain antibody protein therapeutics with the potential to treat some of today’s most challenging medical conditions.
The i-body technology mimics the shape and stability of a unique and versatile antigen binding domain that was discovered initially in sharks and then developed as a human protein. The result is a range of unique proteins capable of interacting with high selectivity, specificity and affinity with previously difficult to access targets such as G-protein coupled receptors (GPCRs) that are implicated in many serious diseases. i-bodies are the first fully human single domain antibody scaffold and the first based on the shark motif to reach clinical trials.
AdAlta has completed Phase I clinical studies for its lead i-body candidate, AD-214, that is being developed for the treatment of Idiopathic Pulmonary Fibrosis (IPF) and other human fibrotic diseases for which current therapies are sub-optimal and there is a high unmet medical need. AdAlta has a second target in discovery research, also in the field of fibrosis and inflammation.
The Company is also entering collaborative partnerships to advance the development of its i‑body platform. It has a collaboration with Carina Biotech to co-develop precision engineered, i-body enabled CAR-T cell therapies (i-CAR-T) to bring new hope to patients with cancer. It has an agreement with GE Healthcare to co-develop i-bodies as diagnostic imaging agents (i‑PET imaging) against Granzyme B, a biomarker of response to immuno-oncology drugs, a program now in pre-clinical development.
AdAlta’s strategy is to maximise the products developed using its next generation i-body platform by internally discovering and developing selected i-body enabled product candidates against GPCRs implicated in fibrosis, inflammation and cancer and partnering with other biopharmaceutical companies to develop product candidates against other classes of receptor, in other indications, and in other product formats.
Further information can be found at: https://adalta.com.au
For more information, please contact:
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Investors
Tim Oldham, CEO & Managing Director Tel: +61 403 446 665 |
Media
IR Department Tel: +61 411 117 774 |
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.
GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for hematological malignancies as well as multiple solid tumors. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation.
GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in Redwood City, California, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn.
For more information, please contact:
GPCR Therapeutics (in Seoul)
DaYoon Kim – Business Development Manager
Tel: +82-2-878-2848
Scius Communications (in London)
Katja Stout
Tel: +447789435990
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Liberi Group Frans Trouwen, CEO and Founder E: FransTrouwen@LiberiGroup.com
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GPCR Therapeutics Expands US Facilities with Relocation to Redwood City
Redwood City, California, September 08, 2022 – GPCR Therapeutics, Inc., a venture-backed clinical stage international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, today announced that to accommodate the expansion of its US subsidiary, it has relocated from incubator space in San Carlos. GPCR’s US operations will be based in new office and laboratory space at 400 Seaport Court, Redwood City, a premier location for biotech research in the San Francisco Bay Area.
GPCR’s founder and CEO, Dr. Dong Seung Seen, said, “We are delighted to be growing in one of the world’s biggest and best biotech clusters, as neighbors to pharma companies including AbbVie and Bristol Myers Squibb, and many other innovation-driven biotech companies.”
GPCR’s CSO and President of US operations, Dr. Pina Cardarelli, said, “We believe our science will lead to the discovery of specific combination drugs that are more efficacious for cancer treatment, thereby leading to better patient outcomes.”
The new US location has over 8,000 square feet covering one floor, dedicated to GPCR’s R&D efforts and will accommodate capabilities in cell culture, protein engineering, computational chemistry, and high-throughput screening. In addition, GPCR’s new site has ample room for growth, as the current team of 10 employees is expected to nearly double over the coming year.
As GPCR expands, it is actively recruiting to its scientific teams to scale up its R&D programs and start clinical trials.
“We will be proud to launch our first human clinical trials, resulting from outstanding work done over many years by our exceptional teams in South Korea and the USA” concluded Dr. Seen.
GPCR Therapeutics has recently become a member of the San Mateo County Chamber of Commerce.
The company will officially open the new US subsidiary on September 15th with a ribbon cutting ceremony at 11:00 a.m.
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Media contacts:
GPCR Therapeutics (in Redwood City)
Seulki Kim
Tel: +1-206-234-3125
GPCR Therapeutics (in Seoul)
DaYoon Kim – Business Development Manager
Tel: +82-2-878-2848
Scius Communications (in London)
Katja Stout
Tel: +447789435990
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.
GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for multiple solid tumors as well as hematological malignancies. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation.
GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, visit gpcr.co.kr and follow us on LinkedIn.
GPCR Therapeutics Expands Scientific Advisory Board
Seoul, South Korea, 28 April 2022 – GPCR therapeutics, Inc., a venture-backed clinical stage international biopharmaceutical company with an innovative approach to drug discovery based on targeting G Protein Coupled Receptors (GPCR) pairs, today announced four appointments to its Scientific Advisory Board (SAB). Dr. Michel Bouvier, Dr. Luisa Salter-Cid, Dr. Omar Nadeem and Dr. Jon Wigginton will provide scientific expertise to support the company’s research and clinical development. GPCR just had a very successful first meeting including all the Scientific Advisory Board.
GPCR’s CEO, DongSeung Seen, said, “We are delighted to welcome our four distinguished new SAB members. They bring a wealth of scientific knowledge which will be of great help in progressing our lead small molecule asset, GPC-100/Burixafor, and advancing our therapies for multiple solid tumours and haematological malignancies. I look forward to working with them all as we discover and develop innovative therapeutics targeting cancer based on the novel science of GPCR heteromers.”
Dr. Michel Bouvier is a professor of Biochemistry and Molecular Medicine and principal investigator at the Institute for Research in Immunology and Cancer (IRIC) of the Université de Montréal, and has been CEO of IRIC since 2014, and was CEO of IRICoR, a non-profit centre of excellence for commercialization and research for 5 years. He is a world-renowned expert in the field of GPCRs. He obtained his B.Sc. in biochemistry and his Ph.D in Neurological Sciences from the Université de Montréal. He was a post-doctoral fellow at Duke University in the laboratory of the Nobel Laureate, Robert J. Lefkowitz.
Dr. Luisa Salter-Cid is a strategic R&D leader with extensive experience managing drug discovery teams. She has significant experience in drug discovery and development. Currently, she is the CSO of Pioneering Medicines at Flagship Pioneering, a life sciences venture capital company that invests in biotechnology, life sciences, and sustainability companies with successful portfolio companies including Moderna. She previously served as CSO for Gossamer Bio, a clinical-stage biopharmaceutical company focused on discovering, acquiring, developing and commercialising therapeutics in various disease areas. She was also the Vice President for Bristol-Myers Squibb leading the Immuno-oncology and Genomics teams. She obtained her B.Sc. in Biology from the University of Lisbon and her Ph.D in Immunology from the University of Miami.
Dr. Omar Nadeem is a Physician in Medical Oncology and specialises in clinical care and investigation in the field of Multiple Myeloma and plasma cell disorders. He is the Clinical Director for Myeloma Cellular Therapies Program at the Dana-Farber Cancer Institute. He obtained his B.Sc. in Biology from the University of Massachusetts and his MD in Medicine from Ross University, Dominica, West Indies.
Dr. Jon Wigginton is a physician-scientist with over 25 years expertise in cancer immunotherapy and oncology drug development, with leadership experience in both academia and industry. He currently serves as Senior Advisor and Chairman of the SAB at Cullinan Oncology, Inc., as well as on the Board of Directors of Sutro Biopharma and Checkmate Pharmaceuticals. Dr. Wigginton previously served as Chief Medical Officer of Cullinan Oncology, Inc., and as Chief Medical Officer at MacroGenics Inc., where he led the company’s clinical development programs. He has also held leadership positions at Bristol Myers Squibb and at Merck & Co. Early in his career, Dr. Wigginton worked at the National Cancer Institute for over 14 years and served as Head of the Investigational Biologics Section in the Center for Cancer Research. He earned his M.D. from the University of Michigan.
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Media contacts:
GPCR Therapeutics (in Seoul)
DaYoon Kim – Business Development Manager
Tel: +82-2-878-2848
Scius Communications (in UK)
Katja Stout
Tel: +447789435990
About GPCR Therapeutics
GPCR Therapeutics, Inc. is a venture-backed, clinical stage international biopharmaceutical company with an innovative approach to developing therapeutics built on its proprietary GPCR data. The company’s proprietary data driven approach has identified over 1,000 GPCR pairs upon which drug screening campaigns can be pursued. Identification of the best GPCR pair to target for specific disease indications and patient subpopulations creates a personalized approach to combination therapy. By targeting the unique pharmacology of GPCR pairs, the company aims to develop life changing treatments for cancer and other diseases.
GPCR Therapeutics has multiple programs in pre-clinical development with the aim of advancing therapies for multiple solid tumors as well as hematological malignancies. The company’s lead small molecule asset, GPC-100/Burixafor, targets CXCR4, one of the most prevalent chemokine GPCRs overexpressed in various cancers. The company has identified that CXCR4 interacts with the beta-2 adrenergic receptor (B2AR), and this GPCR pair presents an alternate signaling pathway that is synergistically dependent on CXCR4 and B2AR activation.
GPCR Therapeutics has its HQ in Seoul, Korea with additional R&D facilities in the San Francisco Bay Area, USA. For more information, please visit gpcr.co.kr or follow us on LinkedIn.