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

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Showing 1 - 10 of 18 results

Polidocanol is a non-ionic surfactant sclerosing agent indicated to treat uncomplicated spider veins and uncomplicated reticular veins in the lower extremity. Polidocanol also is indicated for the treatment of incompetent great saphenous veins, accessory saphenous veins, and visible varicosities of the great saphenous vein system above and below the knee. When administered, polidocanol locally damages blood vessel endothelium. Following the endothelial damage, platelets aggregate at the site and attach to the venous wall eventually resulting in a dense network of platelets, cellular debris, and fibrin that occludes the vessel. Eventually the vessel is replaced by connective fibrous tissue. Adverse reactions include pain in extremity, infusion site thrombosis, contusion/injection site hematoma, limb discomfort and some others.
Methylene blue, also known as methylthioninium chloride, is a medication from WHO's list of essential medicines. Upon administration, methylene blue is converted to leukomethylene blue by erythrocyte methemoblobin reductase in the presence of NADPH. Leukomethylene blue than reduces methemoglobin to oxyhemoglobin, thus restoring oxygen carrying capacity of the blood. Methylene blue is also used as a dye for various diagnostic procedures, for treatment of ifosfamide toxicity and for in vitro staining. Historically, it was used as a photosensitizer for photodynamic therapy for topical treatment of dermatologic or mucocutaneous infections, as an antidote for cyanide poisoning, but these applications are no longer approved. Methylene blue is investigated in clinical trials for treatment of septic shock and Alzheimer's disease.
Status:
Investigational
Source:
INN:elinafide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Elinafide (LU 79553) is a bisintercalating naphthalamide and a topoisomerase II inhibitor has demonstrated a higher binding affinity for DNA and significant antitumour efficacy against a panel of established tumour cell lines, including several multidrug resistant-positive sublines. Elinafide had been in phase II clinical trial for the treatment of ovarian cancer and phase I trials for the treatment of various solid tumours. The major haematological toxicities observed were anaemia and neutropenia. The major non-haematological toxicities observed in the 3-weekly schedule were neuro-muscular presenting clinically as a mixed syndrome of severe weakness (sometimes with pain in both legs), myalgia and arthralgia, asthenia/fatigue/malaise. One fatality was considered related to LU 79553, as the patient had fever and neutropenia. Clinical study of this drug candidate was discontinued due to its neuromuscular dose-limiting toxicity.
Status:
Investigational
Source:
INN:cemadotin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cemadotin (LU103793) is a cytotoxic water-soluble pentapeptide analogue of dolastatin 15. The dolastatin peptides were originally isolated from the shell-less mollusc Dolabella auricularia. Cemadotin blocks cells at mitosis. It exerts its antitumor activity by suppressing spindle microtubule dynamics through a distinct molecular mechanism by binding at a novel site in tubulin. Cemadotin was in phase II clinical trials as a promising cancer chemotherapeutic agent. However, this agent appears to be inactive in the treatment of advanced non-small-cell lung cancer and other tumors and this research has been discontinued.
Status:
Investigational
Source:
NCT00389779: Phase 3 Interventional Completed Hypertension
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Darusentan is an orally active, propanoic acid-based endothelin receptor antagonist (ERA) that selectively blocks endothelin-1 (ET-1) binding to the endothelin type-A (ETA) receptor. Darusentan exhibited subnanomolar binding affinity and approximately 1000-fold selectivity for the ETA receptor in binding experiments conducted in vitro under steady-state conditions. Darusentan is orally bioavailable and, when administered to humans, maximum plasma concentrations are observed within 1–2 h post dosing. The mean elimination half-life is relatively long (>15 h), which is consistent with once-daily dosing. Darusentan is primarily glucuronidated by Phase II enzymes in the liver, and the major route of elimination of Darusentan and its metabolites is via the bile. Some glucuronidated metabolites of Darusentan are also excreted in the urine. Darusentan doses up to 300 mg/day were well tolerated and associated with a manageable safety profile in patients with resistant hypertension (RHTN). The most frequently reported adverse events in Ddarusentan-treated subjects were peripheral edema (17%) and headache (11%), which were mostly mild or moderate in severity. Other commonly reported adverse events in the Darusentan treatment group were sinusitis (8%), dizziness (7%), upper respiratory tract infection (5%) and gastroenteritis (5%). In phase III clinical trial the mean reductions in clinic systolic and diastolic blood pressures were 9/5 mm Hg with placebo, 17/10 mm Hg with Darusentan 50 mg, 18/10 mm Hg with Darusentan 100 mg, and 18/11 mm Hg with Darusentan 300 mg. Unfortunately, phase III clinical trial evaluating Darusentan did not achieve its co-primary efficacy endpoints of achieving a change in systolic and diastolic blood pressure after 14 weeks compared to a placebo. Perhaps for this reason, shortly after the top-line results of this study became known, the sponsor announced that Darusentan would not be developed further for resistant hypertension.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

Triticonazole is a triazole pesticide/fungicide with broad antifungal activity. Like many azole fungicides, triticonazole likely inhibits 14-α demethylase, inhibiting ergosterol production and fungal cell wall synthesis. Additionally, triticonazole may inhibit aromatase.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Nitrothal-isopropyl is a fungicide, used, usually in combination with other fungicides, to control fungal pathogens on a variety of crops including fruit and vegetables. Nitrothal-isopropyl is registered for use in South Africa, Australia and New Zealand but it is not registered by the USA. Nitrothal-isopropyl is protectively active against powdery mildews and used in combination with sulphur or metiram in apples. Combinations of nitrothal-isopropyl with tridemorph greatly increased the effectiveness against Erysiphe cichoracearum on melons. Nitrothal-isopropyl is a selective fungicide applied towards control of the development of many side effects of diseases caused by microorganisms in plant breeding of agricultural crops. It has been applied for the control of Podosphaera leucotricha in apple trees, Phytophthora infestans in tomato and potato, and Septoria apii in celery as well as Bremia lactucae in lettuce cultivation. Nitrothal-isopropyl is also applied as a seed treatment, in order to combat diseases of vegetable and ornamental plants. It is used in forestry for diseases causing needles drooping as well. In humans NT can cause eyes, skin, and respiration system irritation. Nitrothal-isopropyl is classified as a third-class toxicity pesticide for mammals.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)


Ethylhexyl triazone is a PABA-derivative used in sunscreens to absorb UVB radiation. It is marketed as Uvinul T 150 by BASF. Ethylhexyl triazone has an absorption maximum of 314 nm. Ethylhexyl triazone is not approved as an active ingredient in the U.S., but used in rare cases to boost efficacy of some products. Ethylhexyl triazone is approved for use up to 5% in EU and Japan. It blocks UVB and extremely stable, it is the most effective UVB filter. Only small concentrations are required to achieve high SPF value, has good affinity to keratin and completely insoluble in water, making it particularly good choice for water-resistant sunscreens. Very stable in light – ability to filter UV rays remains practically unchanged even when exposed to intense radiation.
Status:
Possibly Marketed Outside US
Source:
NCT00567983: Phase 4 Interventional Completed Disease Progression
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Boscalid is a new pesticide belonging to the class of oxathiin fungicides, also known as carboxamide, carboxin or (carbox) anilide fungicides. U.S. EPA has designated the proposed uses of boscalid as “reduced risk.” Boscalid works by inhibiting mitrochondial respiration and subsequent production of ATP in fungal cells. Boscalid has a new mode of action and is effective against pathogens resistant to other fungicides, including those resistant to sterol inhibitors, dicarboximides, benzimidazoles, anilinopyrimidines, phenylamides and strobilurins.
Status:
Possibly Marketed Outside US
Source:
NCT03980704: Phase 4 Interventional Completed General Surgery
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Topramezone is a pyrazolone herbicide developed by BASF, which is also an HPPD inhibitor, being effective for the control of weeds, which are resistant to glyphosate, triazines, ALS inhibitors and the ACCase inhibitors. Topramezone has a good control efficacy for corn grassy weed and broad-leaf grass worldwide. Topramezone was registered for the first time in Canada in 2006 for application to post-emergence weed removal in cornfield, followed by releases to Latin America, North America, Japan and Germany. In 2009, BASF brought to the Chinese market its Topramezone with the trade name Arietta®. Topramezone is moderately toxic to birds, honey bees, earthworms, fish and aquatic invertebrates. Topramezone strongly inhibited 4-HPPD activity in vitro, with I(50) values of 15 and 23 nM for the enzyme isolated from S. faberi and recombinant enzyme of Arabidopsis thaliana L. respectively.

Showing 1 - 10 of 18 results