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

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Showing 111 - 120 of 2738 results

Status:
Investigational
Source:
NCT04671303: Phase 2 Interventional Completed Lung Cancer
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



AST-1306, also known as Allitinib, is an orally active potent, selective, irreversible inhibitor of the HER family of receptor tyrosine kinases. AST-1306 inhibits the enzymatic activities of wild-type epidermal growth factor receptor (EGFR) and ErbB2 as well as EGFR resistant mutant in both cell-free and cell-based systems. AST1306 potently suppressed tumor growth in ErbB2-overexpressing adenocarcinoma xenograft and FVB-2/N(neu) transgenic breast cancer mouse models. Allitinib is in Phase I clinical trial for the treatment of advanced solid tumors. Serious adverse effects detected were: diarrhea, dehydration and hyperbilirubinemia.
Status:
Investigational
Source:
NCT03525392: Phase 1 Interventional Terminated Pancreatic Ductal Adenocarcinoma
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:sirpiglenastat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00978211: Phase 2 Interventional Completed Neuroendocrine Tumors
(1997)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Edotreotide (SMT487) is a DOTA-containing somatostatin analog. Edotreotide binds with high affinity to somatostatin receptors. Somatostatin receptors are predominantly overexpressed by neuroendocrine tumors. On 15 September 2016, the European Medicines Agency’s Committee for Medicinal Products for Human Use (CHMP) adopted a positive opinion, recommending granting a marketing authorisation for the orphan medicine edotreotide (SomaKit-TOC) intended for use in Positron Emission Tomography (PET) imaging in adult patients with gastro-enteropancreatic neuroendocrine tumours (GEP-NETs). SomaKit TOC was designated as an orphan medicinal product on 19 March 2015. 68Ga-Edotreotide, distributed under the brand name TOCscan® (Sogacin® in Austria/ France), is the companion diagnostic in ITM´s theranostic approach for the treatment of neuroendocrine tumors (NETs). N.c.a. 177Lu-Edotreotide is known as an innovative Targeted Radionuclide Therapy agent with favorable safety profile and promising efficacy. N.c.a. 177Lu-Edotreotide received an Orphan Designation as treatment of gastro-entero-pancreatic neuroendocrine tumors (GEP-NET) based on academic clinical Phase II data suggesting a significant benefit (substantially improved progression-free survival, PFS).
Status:
Investigational
Source:
NCT04486911: Phase 2 Interventional Active, not recruiting Breast Cancer
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02837900: Phase 2 Interventional Completed Knee Osteoarthritis
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:vemircopan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT01327495: Phase 2/Phase 3 Interventional Completed Healthy
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Merrion Pharmaceuticals was developing an oral tablet formulation of acyline, a gonadotropin-releasing hormone (GnRH) antagonist, referred to as MER 104. MER-104 effectively suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH) secretion in man. Acyline has been investigated for the prevention and treatment of hypogonadism and contraception. Injectable forms have been administered successfully in man in Phase II studies as part of a potential contraceptive regimen. MER-104 is an enteric coated acyline tablet developed by Merrion Pharmaceuticals using GIPET™ I technology to enable the oral administration of this decapeptide. The development of acyline appears to have been discontinued.
Status:
Investigational
Source:
INN:ramorelix
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ramorelix is a glycosylated gonadoliberin antagonist patented by Hoechst A.-G. as an anticancer agent. In preclinical studies, a single injection of ramorelix microparticles inhibited tumor progression for only 14 days. This short action is due to a different release profile of the ramorelix microparticles and the different specific activities of peptides incorporated. In the preventive experiments, animals were treated 17 days after DMBA induction before tumor development. Treatment with buserelin implants every 56 days or with buserelin microparticles every 28 days and the treatment with ramorelix microparticles every 7 days prevented the development of tumors. Six weeks after the last injection of ramorelix microparticles a strong tumor progression was seen. There was a clear correlation between peptide release and tumor inhibition. The implants and the microparticles were well tolerated, no tissue reaction or side-effects of ramorelix were seen.
Status:
Investigational
Source:
NCT01987284: Phase 2 Interventional Completed Isolated Systolic Hypertension
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

SER-100 (previously known as ZP120, Ac-RYYRWKKKKKKK-NH2) is a peripherally acting orphanin FQ/nociceptin (ORL-1) receptor agonist that is in development with Serodus Pharmaceuticals for the treatment of Isolated systolic hypertension. SER-100 is a peripherally acting, highly potent and selective NOP receptor partial agonist, which was developed by coupling a chain of six lysine residues to an existing NOP receptor partial agonist hexapeptide, Ac-RYYRWK-NH2 to improve meta-bolic stability. SER-100 has sodium-potassium-sparing aquaretic and anti-natriuretic activity. SER-100 exerts a chronic hypotensive and bradycardic effects in rodents, including models of systemic and pulmonary hypertension. SER-100 produces its cardiovascular effects, at least in part, by inhibition of cardiac and vascular sympathetic activity. In terms of clinical evaluation, SER-100 was originally assessed in a randomized, double-blind, placebo controlled Phase II trial as add-on therapy in patients with sub-acute decompensated chronic heart failure (NCT00283361); how-ever, the clinical development of the peptide for this indication was terminated prematurely due to significant hypotensive activity, primarily on systolic blood pressure (SBP). Nonetheless, as a result of this profound drop in SBP, SER-100 (10 mg, s.c., bid) was investigated in a randomized, placebo-controlled study in patients with treatment-resistant isolated systolic hypertension (NCT01987284) and found to produce a meaningful and long lasting drop in SBP(~7 mmHg) and diastolic (~4 mmHg) blood pressure (DBP),as well as being safe and well-tolerated. FDA has granted an Orphan Drug Designation for SER-100 in pulmonary arterial hypertension (PAH).