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

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Showing 71 - 80 of 364 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.
Status:
Possibly Marketed Outside US
Source:
Cattlyst by Syntex
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Laidlomycin is a polycyclic polyether antibiotic which possesses an inhibitory activity against various mycoplasma species}, and is effective in controlling coccidiosis in chickens. It is also known as selectively inhibiting the migration of hemagglutinin glycoprotein from Golgi apparatus to the cell surface in measles virus). Laidlomycin inhibited growth of some Gram-positive bacteria only at high concentrations such as 50-100 ug/ml, but was not active against Gram-negative bacteria, yeast and fungi even at concentration of 1,000 ug/ml. In broth dilution, laidlomycin was active against several illycoplasmas and most active against the sterol-nonrequiring mycoplasma, Acholeplasma laidlawii. Under the brand name Cattlyst Laidlomycin is indicated for improved feed efficiency and increased rate of weight gain in cattle fed in confinement for slaughter.
Metomidate is a non-barbiturate imidazole which produces a sleepy condition of 20-60 minutes duration without substantial analgesia. Since the beginning of 1997 the use of the hypnotic drug metomidate (Hypnodil) in swine is nor longer allowed. This ban caused a substantial therapeutic deficit for anesthesia in swine. 11C-metomidate may be used with positron emission tomography which can differentiate adrenocortical from nonadrenocortical tumors and a suspected adrenocortical cancer may be characterized and staged before surgery. Metomidate hydrochloride is for the sedation and anesthesia of aquarium and non-food fish species. Aquacalm has been granted Indexed status by the FDA for this purpose.
Status:
Possibly Marketed Outside US
Source:
Robenz by Kantor, S.|Kennett, R.L.Jr.|Waletzky, E.|Tomcufcik, A.S.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Robenidine (l,3-6ts (p-chlorobenzylidenamino) guanidine hydrochloride) is an effective anticoccidial, first introduced by Kantor, Kennett, Waletzky & Tomcufcik (1970). It does not affect the earliest stages in the coccidial life-cycle and its main activity is against the almost mature first generation schizont. It is used as an aid in the prevention of coccidiosis caused by Eimeria mivati, E. brunetti, E. tenella, E. acervulina, E. maxima and E. necatrix in broiler chickens.
Status:
Possibly Marketed Outside US
Source:
TIMEWISE REPAIR VOLU-FIRM EYE RENEWAL CREAM
Source URL:
First approved in 2009

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levomenol, or more formally α-(−)-bisabolol or (-)-alpha-bisabolol was identified as a major constituent of Salvia runcinata essential oil, a plant indigenous to South Africa. This compound exhibits pharmacological properties such as analgesic, antibiotic and anticancer activities. Mutagenicity and genotoxicity of bisabolol have also been investigated. Due to the low toxicity associated with bisabolol the Food and Drug Administration (FDA) has granted this constituent with Generally Regarded as Safe (GRAS) status, which has promoted its use as an active ingredient in several commercial products. Recently provided experiments have shown the anti-amyloidogenic potential and anti-apoptotic property of the α-bisabolol against Aβ25-35 induced neurotoxicity in PC12 cells. This compound prevented the oligomers formation as well as disaggregates the matured fibrils. It is known, that of the multiple etiological factors of Alzheimer's disease (AD), the accumulation of senile plaques (SPs) particularly as Aβ oligomers correlates with the relentlessness cognitive impairment in AD patients and play a vital role in AD pathology. As a conclusion obtained properties of α-bisabolol allowed suggesting, that this compound could be used as an excellent therapeutic drug to combat AD. Besides, anti-cancer activity of α-bisabolol was also studied. α-Bisabolol inhibited invasiveness and motility in pancreatic cancer through kisspeptin 1 receptor (KISS1R) activation. Further investigations are necessary to clarify the precise mechanisms of α-bisabolol activity for clinical application as a novel treatment for pancreatic cancer.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (MIXED)

Conditions:

Bemotrizinol (INN/USAN, INCI bis-ethylhexyloxyphenol methoxyphenyl triazine) is an oil-soluble organic compound that is added to sunscreens to absorb UV rays. It is marketed as Tinosorb S by BASF and as Escalol S by Ashland Inc. Bemotrizinol is a broad-spectrum UV absorber, absorbing UVB as well as UVA rays. It has two absorption peaks at 310 and 340 nm. It is highly photostable. Even after 50 MEDs (minimal erythemal doses) 98.4% remains intact. It helps prevent the photodegradation of other sunscreen actives like avobenzone. Furthermore, its presense can at least partially protect less photostable UV blockers (e.g. UVA-blocker avobenzone) from degradation. It is approved in Europe and Australia but not in the USA. Unlike some other organic sunscreen agents, bemotrizinol has not been shown to have hormone-like (estrogenic) effects in cell cultures. Bemotrizinol appears to be relatively non-toxic and rarely causes skin irritation. However, as with many synthetic chemicals, it is unclear whether bemotrizinol may produce low-level skin damage and/or systemic effects with long-term use.
Status:
Possibly Marketed Outside US
Source:
WOUND and INFECTION MEDICATION by WESTWOOD LABORATORIES, INC.
(2009)
Source URL:
First approved in 2009
Source:
WOUND and INFECTION MEDICATION by WESTWOOD LABORATORIES, INC.
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Status:
Possibly Marketed Outside US
Source:
Salicylic Acid 6 percent by PruGen LLC
(2009)
Source URL:
First approved in 2009

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Possibly Marketed Outside US
Source:
Zyrexal by Vivera Pharmaceuticals, Inc.
(2020)
Source URL:
First approved in 2009
Source:
Integra by U.S. Pharmaceutical Corporation
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)