Piperidine is an azacycloalkane that is cyclohexane in which one of the carbons is replaced by a nitrogen. Although piperidine is a common organic compound, it is an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.
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GSK announces positive headline results from the EAGLE-1 Phase III trial for Gepotidacin in uncomplicated urogenital gonorrhea. Gonorrhoea is the second most common sexually transmitted infection due to the pathogen N. gonorrhoeae. Untreated urogenital gonorrhea can cause serious and permanent health problems, such as pelvic inflammatory disease and infertility.
Gepotidacin is an investigational, first-in-class inhibitor of bacterial topoisomerase. It has a distinct mechanism of action that inhibits bacterial DNA replication by selectively interacting with two key bacterial enzymes, DNA gyrase and topoisomerase IV. Gepotidacin confers activity against most strains of E. coli and S. saprophyticus, and N. gonorrhoeae, including target pathogens resistant to current antibiotics.
Crinetics’ once-daily oral paltusotine achieved the primary and all secondary endpoints in the phase 3 PATHFNDR-2 study in acromegaly patients.
Acromegaly is a serious rare disease generally caused by a pituitary adenoma, a benign tumor in the pituitary that secretes growth hormone (GH). Excess GH secretion causes excess secretion of IGF-1 from the liver. Prolonged exposure to increased levels of IGF-1 and GH leads to progressive and serious systemic complications, often resulting in bone, joint, cardiovascular, metabolic, cerebrovascular, or respiratory disease.
Paltusotine is the first oral, once-daily selectively-targeted somatostatin receptor type 2 (SST2) agonist and is currently in investigational Phase 3 studies for acromegaly and a Phase 2 study for carcinoid syndrome.
Boehringer’s zongertinib shows encouraging efficacy and tolerability profile in previously treated HER2 mutated lung cancer patients.
Zongertinib (also known as BI 1810631) is an investigational oral HER2-specific tyrosine kinase inhibitor (TKI) that is being developed as a potential treatment for HER2 mutated non-small cell lung cancer (NSCLC). Zongertinib was granted FDA Fast Track Designation in 2023, then in 2024 it was granted Breakthrough Therapy Designation by the U.S. FDA and China CDE for the treatment of adult patients with advanced NSCLC whose tumors have activating HER2 mutations, and who have received a prior systemic therapy.
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