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

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Showing 1051 - 1060 of 1085 results

Toceranib (toceranib phosphate) is an orally bioavailable small molecule inhibitor that blocks a variety of RTKs, including VEGFR2, PDGFRa and KIT. In non-clinical pharmacology studies, toceranib selectively inhibited the tyrosine kinase activity of several members of the split kinase receptor tyrosine kinase (RTK) family, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Toceranib inhibited the activity of Flk-1/KDR tyrosine kinase (vascular endothelial growth factor receptor, VEGFR2), platelet-derived growth factor receptor (PDGFR), and stem cell factor receptor (Kit) in both biochemical and cellular assays. Toceranib has been shown to exert an antiproliferative effect on endothelial cells in vitro. Toceranib treatment can induce cell cycle arrest and subsequent apoptosis in tumor cell lines expressing activating mutations in the split kinase RTK, ckit. Canine mast cell tumor growth is frequently driven by activating mutations in c-kit. Toceranib is a dog-specific anti-cancer drug approved by the U.S. Food and Drug Administration. It is marketed as Palladia as its phosphate salt, toceranib phosphate by Pfizer. PALLADIA (Toceranib) tablets are indicated for the treatment of Patnaik grade II or III, recurrent, cutaneous mast cell tumors with or without regional lymph node involvement in dogs.
Adenine is a nucleobase (a purine derivative). Its derivatives have a variety of roles in biochemistry including cellular respiration, in the form of both the energy-rich adenosine triphosphate (ATP) and the cofactors nicotinamide adenine dinucleotide (NAD) and flavin adenine dinucleotide (FAD). It also has functions in protein synthesis and as a chemical component of DNA and RNA. The shape of adenine is complementary to either thymine in DNA or uracil in RNA
Status:
Possibly Marketed Outside US
Source:
Canada:ETHOXYQUIN
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Ethoxyquin (EQ) has been used as an antioxidant in animal feed for many years, but pharmacological use of EQ has never been evaluated in humans despite that small amounts of EQ exist in certain food items. The level of this antioxidant in animal feeds should not be higher than 150 ppm (U.S. FDA permissions). Ethoxyquin is rapidly absorbed from gastrointestinal tract of laboratory animals like rats and mice. Peak blood concentration of the compound is observed within 1 h. Distribution of EQ in animal body is similar when it is administered orally and intravenously. Small amounts of parent EQ were detected in liver, kidney, and adipose tissue and fish muscles. It is excreted predominantly as metabolites via urine. Ethoxyquin is also registered as an antioxidant to control scald (browning) in apples and pears. EQ-induced DNA damage in human lymphocytes in a dose-dependent manner. According to the studies on dogs and laboratory animals it was shown that ethoxyquin had little acute toxicity, except when it is administered parenterally. Values of LD50 for EQ are 1700 mg kg−1 bw (rats, oral gavage), 2000 mg kg−1 bw (rats, dermal treatment, 24 h), 900 mg kg−1 bw (mice, intraperitoneal administration), and 180 mg kg−1 bw (mice, intravenous administration).
Status:
Possibly Marketed Outside US
Source:
Schmerz. Apr 2003;17(2):110-6.: Phase 4 Human clinical trial Completed Pain, Postoperative
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

TILIDINE is a low to medium potency opioid analgesic. It is metabolized to its active metabolites, nortilidine and bisnortilidine. Its analgesic activity is largely exerted through nortilidine which is a potent agonist at Mu opioid receptors.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)


Oxolamine under brand names Symphocal, Perebron is used in some countries as a cough suppressant for the treatment of pharyngitis, tracheitis, bronchitis, bronchiectasis, pertussis. Oxolamine possesses anti-inflammatory activity, which causes a reduction in the irritation of the nervous receptors of the respiratory tract.
Vinburnine is a nutritional product, a peripheral vasodilator with cerebral activities that also act as a cerebral metabolic stimulant and appears to be able to relax the smooth muscle cells within the walls of blood vessels. (+/-)-Eburnamonine is the racemate of the alkaloid Vinburnine. Dextrorotatory, levorotatory, and racemic forms of eburnamonine exist in nature. The (-)-form, also known as vincamone (isolated from Vinca minor), is a drug that possesses a stimulating activity for muscle and is used as cerebrotonic, whereas both enantiomers have hypotensive effects.
Piperaquine is a bisquinoline antimalarial drug that was first synthesized in the 1960s and used extensively in China and Indochina as prophylaxis and treatment during the next 20 years. Usage declined in the 1980s as piperaquine-resistant strains of P. falciparum arose and artemisinin-based antimalarials became available. However, during the next decade, piperaquine was rediscovered by Chinese scientists as one of a number of compounds suitable for combination with an artemisinin derivative. The rationale for such artemisinin combination therapies (ACTs) was to provide an inexpensive, short-course treatment regimen with a high cure rate and good tolerability that would reduce transmission and protect against the development of parasite resistance. Piperaquine is characterized by slow absorption and a long biological half-life, making it a good partner drug with artemisinin derivatives which are fast acting but have a short biological half-life.
Status:
Possibly Marketed Outside US
Source:
NCT02213068: Phase 4 Interventional Completed Transplant; Failure, Kidney
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Aminopropyl racementhyl phosphate is a prodrug of menthol patented by Pacific Corporation (Korea). Upon administration, it is enzymatically decomposed into menthol and 3-aminopropylphosphoric acid, a component used for anti-aging cosmetic composition. Aminopropyl racementhyl phosphate was found to reduce the irritation of menthol while maintaining its useful effects.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Isaxonine (N-isopropyl-amino-2-pyrimidine orthophosphate) is able to accelerate nerve regeneration and functional recovery. Isaxonine has specific affinity for peripheral nerves. It acts directly on the neuron or indirectly by stimulating the production of a growth factor remains unknown. It demonstrates activity in the treatment of neuropathies of various etiology. Isaxonine treatment may be associated with hepatotoxicity.
Status:
Possibly Marketed Outside US
Source:
NCT01930331: Phase 4 Interventional Completed Plasmodium Falciparum
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Naphthoquine is an antimalarial drug first synthesized in China in 1986 but which was not developed for clinical use until the late 1990s. This drug now is used in combination for treatment of Plasmodium Falciparum and Malaria. The use of anti-malarial drug combinations with artemisinin or with one of its derivatives is now widely recommended to overcome drug resistance in falciparum as well as vivax malaria. The fixed oral dose artemisinin-naphthoquine combination (ANQ, ARCO™) is a newer artemisinin-based combination (ACT) therapy undergoing clinical assessment.

Showing 1051 - 1060 of 1085 results