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

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Showing 81 - 90 of 2696 results

Status:
Investigational
Source:
USAN:FOSBRETABULIN TROMETHAMINE [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Combretastatin A4 is a vascular disrupting agent (VDA) that targets tumor vasculature to inhibit angiogenesis. Combretastatin A4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin and inhibits tubulin assembly. This tubulin-binding agent was originally isolated from an African shrub, Combretum caffrum. Combretastatin A4 is cytotoxic to umbilical-vein endothelial cells (HUVECs) and to a range of cells derived from primary tumors and these cytotoxicity profiles have been used to assess several novel analogs of the drug for future development. Combretastatin A4 has antitumor activity by inhibiting AKT function. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability. Several studies in mice have shown that a single administration of combretastatin A4 (100 mg/kg) does not significantly affect primary tumor growth. However, repeated administration (12.5 – 25.0mg/kg twice daily) for periods of 10 – 20 days resulted in approximately 50% retardation of growth of ectopic Lewis lung carcinoma and substantial growth delay of T138 spontaneous murine breast tumors. In clinical studies, Combretastatin A4 has been well tolerated in patients at doses up to 56 mg/m2, following a protocol of five daily 10-minute intravenous infusions every 21 days. The disodium combretastatin A4 phosphate prodrug is currently undergoing clinical trials in the UK and USA.
Status:
Investigational
Source:
INN:dexfadrostat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



(+)-Fadrozole (FAD-286) is an aldosterone synthase inhibitor. The drug was tested in vivo in preclinical models of hypertension, heart failure and was shown to reduce retinal neovascularization in rats with oxygen-induced retinopathy.
Status:
Investigational
Source:
JAN:TOLVAPTAN SODIUM PHOSPHATE [JAN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

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

Class (Stereo):
CHEMICAL (RACEMIC)

Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.
Status:
Investigational
Source:
INN:fosquidone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Fosquidone (also known as GR63178A), a pentacyclic pyrroloquinone that was developed as an anticancer agent. Fosquidone participated in phase II clinical trial for the treatment of patients with colorectal, renal and non-small cell lung cancer. However, the drug didn’t show significant antitumor activity. The further development of this drug was discontinued.
Status:
Investigational
Source:
INN:fospirate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fospirate is an organophosphorus insecticide used in veterinary as an anthelmintic agent.
Lisofylline [1-(5R-hydroxyhexyl)-3,7-dimethylxanthine] is a unique metabolite of pentoxifylline. Lisofylline inhibited the generation of phosphatidic acid and free fatty acids. Lisofylline blocked the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy and in experimental sepsis. Lisofylline regulates immune cell function and autoimmune response by inhibition of IL-12 signalling and cytokine production. Lisofylline may have therapeutic value in the prevention of autoimmune disorders, including Type 1 diabetes, autoimmune recurrence following islet transplantation, and in preservation of beta cell functional mass during islet isolation.
Status:
Investigational
Source:
INN:vibozilimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Vapendavir (BTA-798) is an orally active capsid-binding inhibitor. It is a potent, orally bioavailable, broad spectrum inhibitor of the large group of HRVs. Vapendavir binds tightly to VP1s canyon and disrupts the ability of the capsid to bind to a specific cell surface receptor. This further inhibits the release of the viral RNA into the cell cytoplasm during the viral uncoating process (removing the lipid bilayer), thereby disrupting viral replication. Vapendavir is designed to be dosed orally. Vapendavir is in phase II clinical trials for the treatment of rhinovirus-induced aggravation of pre-existing asthma or COPD. Vapendavir has shown significant results in proof-of-concept studies. Thus far, from the Phase 1/2 studies conducted, vapendavir has demonstrated a desirable clinical pharmacology profile with high bioavailability, linear pharmacokinetic profile, remained unaffected by concomitant medications, and was not exclusively metabolized.
Status:
Investigational
Source:
INN:icanbelimod [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)