First selective small molecule ephrin receptor kinase inhibitor to enter development
GLPG1790 has high efficacy against triple-negative breast cancer
Potentially suitable for other ephrin-driven cancers
GLPG1790 is fully proprietary to Galapagos
Mechelen, Belgium; 18 March 2014 – Galapagos NV (Euronext: GLPG) will present favorable pre-clinical data on GLPG1790 in triple-negative breast cancer at the American Association for Cancer Research (AACR) Annual Meeting in San Diego on 7 April 2014. In the abstract, Galapagos disclosed that GLPG1790 is the first selective small molecule inhibitor of the ephrin receptor kinase family, which could play a key role in melanoma, pancreatic, ovarian, prostatic, and colorectal cancers, in addition to triple-negative breast cancer.
“With GLPG1790, Galapagos shows once again that it excels in identification of relevant novel modes of action, and is successful in discovering selective compounds directed toward these,” says Dr Piet Wigerinck, Galapagos CSO. “We are pleased to present the ephrin receptor kinase targeted approach of GLPG1790 towards triple-negative breast and potentially other ephrin-driven cancers at AACR this year. Targeted approaches in oncology typically show good efficacy and less toxicity than chemotherapy.”
AACR poster details
Abstract number: 1753
Poster session: 7 April 2014, 8 AM – 12 PM, Hall A-E, Poster Section 31, Poster #26
“GLPG1790: the first Ephrin (EPH) receptor tyrosine kinase inhibitor for the treatment of triple negative breast cancer”
Candidate drug GLPG1790 shows remarkable in vivo efficacy in a triple negative breast cancer xenograft pre-clinical model. Full tumor blockage was observed after 30 mg/kg/d oral dosing, correlated with target inhibition in the tumor. Extensive molecular mode of action studies, using GLPG1790 and knock-down tools, prove EPHA2 target engagement and impact on the MAPK pathway and cell cycle, important elements of the biology of many cancer types.
GLPG1790 has good drug-like properties, and safety/tolerability studies with the candidate drug look favorable. Galapagos is completing preclinical studies with GLPG1790, and is carefully considering a number of options before entering the first clinical trials in humans. This novel program is fully proprietary to Galapagos.
About triple-negative breast cancer
GLPG1790 has shown high activity against breast tumors that are triple-negative, for which the absence of estrogen (ER), progesterone (PR) or HER2 receptors affects the prognosis for recovery, and no targeted therapeutic options are currently available. Breast cancer is a disease in which tumor cells form in the breast tissue; it is one of the most common types of cancer in women. There are many different types of breast cancer, and as a result, there are many options for treatment. Targeted drug treatments such as Herceptin® and Avastin®attack specific types of breast cancer cells. Decisions about the best possible treatment with targeted drugs are based on tests for the presence of ER, PR and HER2. Triple-negative breast cancer (tumor cells that have no ER, PR and HER2) accounts for one-fifth of breast cancers, and it usually affects young women. There are no targeted drugs available yet for patients with triple-negative breast cancer.
Galapagos (Euronext: GLPG; OTC: GLPYY) is specialized in novel modes-of-action, with a large pipeline comprising five Phase 2 studies (two led by GSK), one Phase 1 study, six pre-clinical, and 20 discovery small-molecule and antibody programs in cystic fibrosis, inflammation, antibiotics, metabolic disease, and other indications. In the field of inflammation, AbbVie and Galapagos signed a worldwide license agreement whereby AbbVie will be responsible for further development and commercialization of GLPG0634 after Phase 2B. GLPG0634 is an orally-available, selective inhibitor of JAK1 for the treatment of rheumatoid arthritis and potentially other inflammatory diseases, currently in Phase 2B studies in RA and in Phase 2 in Crohn’s disease. Galapagos has another selective JAK1 inhibitor in Phase 2 in ulcerative colitis and psoriasis, GSK2586184 (formerly GLPG0778, in-licensed by GlaxoSmithKline in 2012). GLPG0974 is the first inhibitor of FFA2 to be evaluated clinically for the treatment of IBD; this program is currently in a Proof-of-Concept Phase 2 study. GLPG1205 is a first-in-class molecule that targets inflammatory disorders and has completed Phase 1. AbbVie and Galapagos signed an agreement in CF whereby they work collaboratively to develop and commercialize oral drugs that address two mutations in the CFTR gene, the G551D and F508del mutation. Potentiator GLPG1837 is at the pre-clinical candidate stage. Galapagos has 400 employees, operating from its Mechelen, Belgium headquarters and facilities in The Netherlands, France, and Croatia. Further information at: www.glpg.com
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Herceptin® and Avastin® are registered trademarks of Roche for trastuzumab and bevacizumab, respectively
Human epidermal growth factor type 2 receptor