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

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Showing 551 - 560 of 21518 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02452346: Phase 2 Interventional Completed Myelodysplastic Syndrome
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tosedostat is a proprietary orally bioavailable inhibitor of the M1 family of aminopeptidases with potential antineoplastic activity. Tosedostat is converted intracellularly into a poorly membrane-permeable active metabolite (CHR-79888) which inhibits the M1 family of aminopeptidases, particularly puromycin-sensitive aminopeptidase (PuSA), and leukotriene A4 (LTA4) hydrolase; inhibition of these aminopeptidases in tumor cells may result in amino acid deprivation, inhibition of protein synthesis due to a decrease in the intracellular free amino acid pool, an increase in the level of the proapoptotic protein Noxa, and cell death. There are several ongoing Phase 2 cooperative group-sponsored trials and investigator-sponsored trials evaluating the clinical activity of Tosedostat in combination with standard agents in patients with acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS).
Arhalofenate is a uricosuric drug which lowers serum urate by blocking its reabsorption by the proximal tubules of the kidney. Arhalofenate activity is mediated by inhibition of URAT1, OAT4 and OAT10. Additionally, arhalofenate has been suggested to exert potent anti-inflammatory activity. Arhalofenate has completed Phase 2 and is ready to advance to Phase 3 as a novel potential treatment for gout. The drug was also tested in patients with type 2 diabetes mellitus (phase III study), where it demonstrated its ability to lower glucose level, acting as a selective, partial PPAR-gamma agonist. However, the development of arhalofenate as an anti-diabetic drug was terminated.
Status:
Investigational
Source:
NCT04580394: Phase 2 Interventional Completed Obstructive Sleep Apnea
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (EPIMERIC)

Status:
Investigational
Source:
NCT02649790: Phase 1/Phase 2 Interventional Completed Relapsed/Refractory Multiple Myeloma (RRMM)
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:

Eltanexor (KPT-8602) is an investigational second-generation Selective Inhibitor of Nuclear Export (SINE) compound that is designed to selectively block the nuclear export protein XPO1. Most of the key tumor suppressor proteins (TSPs), are cargos of XPO1 and inhibition of XPO1 by eltanexor is believed to sequester TSPs in the nucleus where they can carry out their normal functions. Karyopharm Therapeutics is developing eltanexor for the treatment of relapsed/refractory cancers.
Status:
Investigational
Source:
INN:gintemetostat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02759601: Phase 1/Phase 2 Interventional Unknown status Hepatocellular Carcinoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tefinostat (also known as CHR-2845) was developed as an innovative oral HDAC (histone deacetylase) inhibitor that selectively targets macrophages and monocytes – central cells of the innate immune system. Chroma Therapeutics develops tefinostat for the treatment of hematological and lymphoid malignancies. In addition, the drug is under investigation in clinical trial phase I/II for cancer-associated inflammation in hepatocellular carcinoma. The aim of this study is to find the best dose of the drug without causing side effects. Besides, Phase II of clinical trial ‘MONOCLE’ study for the treatment of chronic myelomonocytic leukemia (CMML) has been initiated and the first patient has been recruited.