— First Drug Candidate to Block Primary RET Fusion and Secondary Predicted Mutations and Induce Tumor Regression —
— Novel discovery demonstrates RET fusions drive tumor growth in breast and colon cancers —
CAMBRIDGE, MA, USA I June 22, 2015 I Blueprint Medicines today announced the first preclinical data for its drug candidate BLU6864, a RET-specific kinase inhibitor. In preclinical studies, BLU6864 induced tumor regression in disease models driven by the primary RET fusion and all predicted secondary resistance mutations. RET is a key disease driver in multiple cancers. These data were presented at the EACR-AACR-SIC Special Conference on Anticancer Drug Action and Drug Resistance in Florence, Italy.
“One of the greatest challenges in treating cancer is cancer cell’s ability to mutate and become resistant to treatment,” said Alexander Drilon, M.D., a medical oncologist at Memorial Sloan Kettering Cancer Center. “RETfusions fuel the development and growth of multiple cancers, including lung and thyroid cancers. By targeting both the main cancer driver and predicted resistance mutations that arise from targeted therapy, we hope to provide patients with transformative medicines that mount a more effective attack on this subset of cancers and prevent recurrences of the disease.”
In the preclinical data presented at the EACR-AACR-SIC Special Conference, BLU6864:
- Inhibited tumor growth and induced tumor regression at well-tolerated doses in a model of cancer driven by RET fusions,
- Inhibited tumor growth and induced tumor regression in a model harboring a resistance mutation that renders cancer cells insensitive to treatment with an approved multi-kinase inhibitor with activity against RET, and
- Spared VEGFR2, a kinase often inhibited together with RET and whose inhibition is associated with dose-limiting toxicities.
BLU6864 is one of the first kinase inhibitors designed specifically to inhibit RET. The drug candidate builds on Blueprint Medicines’ work to identify novel drivers of disease. In addition to lung and thyroid cancers, the Company’s scientists discovered that RET fusions are drivers in a subset of colon and breast tumors. Leveraging its expertise in genomics and structural biology, Blueprint Medicines was able to predict and validate the complete spectrum of future resistance mutations and designed drug candidates to target both the primary RET fusions and secondary treatment-resistant mutants.
In addition to BLU6864, Blueprint Medicines has two drug candidates on track to begin Phase 1 clinical trials in mid-2015, including BLU-554 in hepatocellular carcinoma and BLU-285 in metastatic and treatment-resistant gastrointestinal stromal tumors as well as systemic mastocytosis.
About Blueprint Medicines
Blueprint Medicines makes kinase drugs to treat patients with genomically defined diseases. Led by a team of industry innovators, Blueprint Medicines integrates a novel target discovery engine and a proprietary compound library to understand the blueprint of cancer and craft highly selective therapies. This empowers the Blueprint Medicines team to develop patient-defined medicines aimed at eradicating cancer.
SOURCE: Blueprint Medicines
Post Views: 108
— First Drug Candidate to Block Primary RET Fusion and Secondary Predicted Mutations and Induce Tumor Regression —
— Novel discovery demonstrates RET fusions drive tumor growth in breast and colon cancers —
CAMBRIDGE, MA, USA I June 22, 2015 I Blueprint Medicines today announced the first preclinical data for its drug candidate BLU6864, a RET-specific kinase inhibitor. In preclinical studies, BLU6864 induced tumor regression in disease models driven by the primary RET fusion and all predicted secondary resistance mutations. RET is a key disease driver in multiple cancers. These data were presented at the EACR-AACR-SIC Special Conference on Anticancer Drug Action and Drug Resistance in Florence, Italy.
“One of the greatest challenges in treating cancer is cancer cell’s ability to mutate and become resistant to treatment,” said Alexander Drilon, M.D., a medical oncologist at Memorial Sloan Kettering Cancer Center. “RETfusions fuel the development and growth of multiple cancers, including lung and thyroid cancers. By targeting both the main cancer driver and predicted resistance mutations that arise from targeted therapy, we hope to provide patients with transformative medicines that mount a more effective attack on this subset of cancers and prevent recurrences of the disease.”
In the preclinical data presented at the EACR-AACR-SIC Special Conference, BLU6864:
- Inhibited tumor growth and induced tumor regression at well-tolerated doses in a model of cancer driven by RET fusions,
- Inhibited tumor growth and induced tumor regression in a model harboring a resistance mutation that renders cancer cells insensitive to treatment with an approved multi-kinase inhibitor with activity against RET, and
- Spared VEGFR2, a kinase often inhibited together with RET and whose inhibition is associated with dose-limiting toxicities.
BLU6864 is one of the first kinase inhibitors designed specifically to inhibit RET. The drug candidate builds on Blueprint Medicines’ work to identify novel drivers of disease. In addition to lung and thyroid cancers, the Company’s scientists discovered that RET fusions are drivers in a subset of colon and breast tumors. Leveraging its expertise in genomics and structural biology, Blueprint Medicines was able to predict and validate the complete spectrum of future resistance mutations and designed drug candidates to target both the primary RET fusions and secondary treatment-resistant mutants.
In addition to BLU6864, Blueprint Medicines has two drug candidates on track to begin Phase 1 clinical trials in mid-2015, including BLU-554 in hepatocellular carcinoma and BLU-285 in metastatic and treatment-resistant gastrointestinal stromal tumors as well as systemic mastocytosis.
About Blueprint Medicines
Blueprint Medicines makes kinase drugs to treat patients with genomically defined diseases. Led by a team of industry innovators, Blueprint Medicines integrates a novel target discovery engine and a proprietary compound library to understand the blueprint of cancer and craft highly selective therapies. This empowers the Blueprint Medicines team to develop patient-defined medicines aimed at eradicating cancer.
SOURCE: Blueprint Medicines
Post Views: 108
