Piperazine is an organic compound consisting of a six-membered ring containing two nitrogen atoms in opposite positions in the ring. The chemical formula of piperazine is C4H10N2, and it is an important pharmaceutical intermediate. Pyrimidines and piperazines are known to be the backbone of many bulk compounds and important core structures for approved drugs; studies have shown that combining a pyridine ring with a piperazine moiety within a single structural framework enhances biological activity.
Sept. 06, 2023, positive feedback from the U.S. FDA and the EU EMA on key elements of the trial design for PROPEL3, its pivotal Phase 3 study of infigratinib in children with achondroplasia.
Achondroplasia is the most common cause of disproportionate short stature, affecting approximately 55,000 people in the United States and European Union, including up to 10,000 children and adolescents with open growth plates. Achondroplasia impacts overall health and quality of life, leading to medical complications such as obstructive sleep apnea, middle ear dysfunction, kyphosis, and spinal stenosis. The condition is uniformly caused by an activating mutation in FGFR3.
Infigratinib is an oral small molecule designed to inhibit FGFR3 and target achondroplasia at its source. It is incredibly exciting that infigratinib has the potential to become the first effective oral treatment option to improve growth, enhance functionality and decrease complications.
Nuvectis Pharma announces encouraging preliminary data from the NXP800 phase 1b clinical trial in platinum-resistant ARID1a-mutated ovarian cancer. There is a 33% response rate and 100% disease control rate in patients evaluated for efficacy.
Heat shock transcription factor 1 (HSF1) is critical for tumorigenesis and progression, and is implicated in multiple solid tumors. NXP800 is a potent, clinical stage inhibitor of the HSF1 pathway. The compound activates GCN2 kinase, that phosphorylates the eIF2α and later encodes the ATF4 transcription regulator, resulting in cancer cell death. NXP800 previously gets Fast Track Designation for platinum-resistant, ARID1a-mutated ovarian cancer.
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