U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 511 - 520 of 530 results

Triptorelin is a synthetic decapeptide agonist analog of luteinizing hormone releasing hormone (LHRH). It works by decreasing the production of certain hormones, which reduces testosterone levels in the body. Animal studies comparing triptorelin to native GnRH found that triptorelin had 13 fold higher releasing activity for luteinizing hormone, and 21-fold higher releasing activity for follicle-stimulating hormone. Triptorelin is indicated for the palliative treatment of advanced prostate cancer.
Teriparatide was manufactured under the brand name FORTEO. FORTEO contains recombinant human parathyroid hormone (1-34), [rhPTH(1-34)], which has an identical sequence to the 34 N-terminal amino acids (the biologically active region) of the 84-amino acid human parathyroid hormone, that regulates calcium and phosphate in the body. FORTEO is indicated for the treatment of postmenopausal women with severe osteoporosis who are at high risk of fracture or who have failed or are intolerant to previous osteoporosis therapy. In addition, Forteo is used for the treatment of osteoporosis associated with sustained systemic glucocorticoid therapy in men and women who are at increased risk for fracture. The biological actions of teriparatide is mediated through binding to specific high-affinity cell-surface receptors. Teriparatide is not expected to accumulate in bone or other tissues.
Cosyntropin (ACTH (1–24)) is a synthetic peptide that is identical to the 24-amino acid segment at the N-terminal of adrenocorticotropic hormone. It is intended for use as a diagnostic agent in the screening of patients presumed to have adrenocortical insufficiency. Cosyntropin may bind to sites located on the adrenergic nerve endings associated with the cardiac tissue, and such binding would interfere with the neuronal reuptake of the catecholamines
Delcasertib is a peptide inhibitor of protein kinase C-delta, developed by KAI Pharmaceuticals. Delcasertib disrupts binding of delta-PKC to its receptor for activated C kinase, thereby preventing localization of delta-PKC to the mitochondria during periods of myocardial ischemia and reperfusion. In preclinical studies, when given as a single intracoronary dose, delcasertib reduced infarct size, enhanced early recovery of regional left ventricular contractility, and improved microvascular patency and function in animal models of acute myocardial infarction. The compound diminished myocardial necrosis and improved reperfusion in a pilot study during the primary percutaneous coronary intervention (PCI) for ST-elevation myocardial infarction (STEMI). In a larger clinical trial, however, intravenous infusion of delcasertib during PCI for acute STEMI in a population of patients treated according to the contemporary standard of care did not reduce biomarkers of myocardial injury.
Forigerimod (also known as IPP-201101) a phosphopeptide is being investigated for the treatment of Lupus Erythematosus, Systemic. This drug is completed phase III clinical trials and is ready for licensing.
Anaritide (Auriculin-Registered Trademark) is a 25-amino-acid synthetic form of atrial natriuretic peptide. Scios Nova was developing anaritide acetate for use in the treatment, prevention and diagnosis of acute renal failure, heart failure and hypertension. Scios suspended development of AURICULIN® anaritide based upon the results of an interim analysis of data from a 250-patient Phase III study in oliguric acute renal failure. The study was suspended due to the low probability that a positive outcome could be obtained with respect to its primary clinical endpoint, dialysis-free survival.
N-(2-Bromophenyl)-9-Methyl-9-Azabicyclo[3.3.1]Nonan-3-Amine (also known as AT-1001) is a high-affinity and highly selective ligand at α3β4 nicotinic cholinergic receptors (nAChRs) that was reported to decrease nicotine self-administration in rats. AT-1001 has a single-digit nanomolar binding affinity for the α3β4 nAChR and over 100-fold selectivity over the α4β2 nAChR and α7 nAChR in competition binding experiments. In electrophysiological experiments, AT-1001 had partial agonist activity at the α3β4 nAChR, evoking 35% of maximum ACh response, and at the same doses, produced desensitization of the ACh response, effectively acting as a functional antagonist at the α3β4 nAChR. Interestingly, AT-1001 also selectively decreased self-administration of cigarette smoke extract (CSE), an aqueous extract of cigarette smoke components, without altering natural food intake, when administered systemically to rats trained to self-administer CSE
Rusalatide acetate (also known as chrysalin or TP 508) is a 23-amino acid peptide derived from human prothrombin; it represents part of the receptor-binding domain of the human thrombin molecule. Rusalatide acetate binds to high-affinity thrombin receptors and mimics cellular effects of thrombin at sites of tissue injury. Rusalatide acetate demonstrated safety and potential efficacy in phase I/II clinical trials for the treatment of diabetic foot ulcers. It interacts with cell surface receptors to stimulate a cascade of cellular and molecular wound healing events, including activation of nitric oxide signaling. In addition, this drug participated in phase II clinical trial to determine the effectiveness of four doses for treating broken wrists in adults. However, this study was terminated because the drug did not demonstrate benefit compared to placebo. Rusalatide acetate was also studied as a cardiovascular drug. However, in January 2012, Capstone discontinued the development of rusalatide, for financial reasons. Recent studies show that a single injection of TP508 (rusalatide acetate) administered 24 h after irradiation significantly increases survival and delays mortality in murine models of acute radiation mortality. Thus, this drug is being developed as a potential nuclear countermeasure.
Peginesatide (trade name Omontys, formerly Hematide), developed by Affymax and Takeda, is an erythropoietic agent, a functional analog of erythropoietin. It was approved by the U.S. Food and Drug Administration for treatment of anemia associated with chronic kidney disease (CKD) in adult patients on dialysis. Peginesatide is a synthetic peptide, attached to polyethylene glycol ("PEGylated"). It mimics the structure of erythropoietin, the human glycoprotein which promotes red blood cell development. Peginesatide binds to and activates the human erythropoietin receptor and stimulates erythropoiesis in human red cell precursors in vitro.

Showing 511 - 520 of 530 results