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

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Showing 111 - 120 of 523 results

Status:
Investigational
Source:
NCT03216499: Phase 2 Interventional Completed Recurrent Glioblastoma
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Motesanib (AMG 706), a novel nicotinamide, was identified as a potent, orally bioavailable inhibitor of the VEGFR1/Flt1, VEGFR2/kinase domain receptor/Flk-1, VEGFR3/Flt4 and Kit receptors. Motesanib was expected to reduce vascular permeability and blood flow in human tumours. A phase III trial of motesanib in combination with paclitaxel and carboplatin in non-squamous NSCLC has been terminated by Takeda and subsequently the development was discontinued. Motesanib has also been investigated up to phase II in breast, thyroid, colorectal and gastrointestinal stromal tumours. However, development has been discontinued in these indications.
Status:
Investigational
Source:
NCT02890173: Phase 3 Interventional Completed Essential Hypertension
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT02073838: Phase 2 Human clinical trial Completed Leukemia, Myeloid, Acute/genetics/metabolism
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
NCT03681093: Phase 3 Interventional Completed Nasal Polyps
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Fevipiprant is a selective reversible antagonist of the prostaglandin D2 receptor (also known as CRTH2). It is currently in development for the treatment of allergic diseases.
Status:
Investigational
Source:
NCT04327024: Phase 2 Interventional Completed Heart Failure With Preserved Ejection Fraction (HFpEF)
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Verinurad (RDEA3170) is a selective uric acid reabsorption inhibitor in clinical development for the treatment of gout and asymptomatic hyperuricemia. Verinurad specifically inhibits URAT1 with a potency of 25 nM. High affinity inhibition of uric acid transport requires URAT1 residues Cys-32, Ser-35, Phe-365 and Ile-481. Unlike other available uricosuric agents, the requirement for Cys-32 is unique to verinurad. Verinurad doses as low as 2.5 mg produce significant sUA lowering in humans, and this greater reduction in sUA may lead to improved outcomes and medical benefits for patients with gout. Verinurad in monotherapy studies has been associated with increased urinary uric acid concentrations and low rates of serum creatinine (sCr) elevation. Verinurad combined with febuxostat decreased sUA dose-dependently while maintaining uric acid excretion similar to baseline. All dose combinations of verinurad and febuxostat were generally well tolerated.
Status:
Investigational
Source:
NCT01935960: Phase 1 Interventional Completed Healthy Subject
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

9cUAB30 is a synthetic analog of 9-cis-RA with little or no RAR-binding activity relative to 9-cis-RA and other RA. 9cUAB30, is a selective rexinoid for the retinoid X nuclear receptors (RXR). Retinoid 9cUAB30 binds to and activates retinoid X receptor (RXR) homodimers and/or and retinoic acid receptor (RAR)/RXR heterodimers, which may result in the dissociation of corepressor protein and the recruitment of coactivator protein, followed by transcription of downstream target genes into mRNAs and protein translation. Gene transcription regulated by these transcription factors may result in inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells. 9cUAB30 displays substantial chemopreventive capacity with little toxicity and is being translated to the clinic as a novel cancer prevention agent. 9cUAB30 has been assessed in vitro with human cell cultures. Human hepatocytes demonstrated no signs of cytotoxicity with treatment of 9cUAB30 up to 50 umol/L, although when human breast cancer cells were treated with 9cUAB30, they showed a significant inhibition of cell proliferation and apoptotic levels 2.5to 3.5 times the levels of untreated cells. 9cUAB30 inhibits telomerase and induces apoptosis in HL60 cells.
Status:
Investigational
Source:
INN:fosalvudine tidoxil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Heidelberg Pharma Research developed fosalvudine tidoxil, a prodrug derived from the nucleoside reverse transcriptase inhibitor alovudine, for the treatment of HIV infections. This drug had reached phase II clinical trials before its development was discontinued.
Status:
Investigational
Source:
NCT01111955: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
NCT01678755: Phase 2 Interventional Completed Schizophrenia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Showing 111 - 120 of 523 results