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

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Showing 41 - 50 of 52 results

AT-9283 was being developed by Astex Pharmaceuticals as a treatment for cancer and myelofibrosis. AT-9283 is an inhibitor of mitosis (cell division) and is the second most progressed drug candidate in the Astex portfolio of novel molecularly targeted cancer drugs. All of Astex’s current products have been discovered internally using its proprietary drug discovery approach. AT9283 is a potent inhibitor of the Aurora A and B kinases and has been shown to arrest tumour growth in a range of tumour models. Aurora kinases play a key role in mitotic checkpoint control in cell division. Both Aurora A and B are over-expressed in many human tumours and are believed to be excellent targets for anti-cancer therapy.
Dovitinib is an orally active small molecule that exhibits potent inhibitory activity against multiple receptor tyrosine kinases (RTK) involved in tumor growth and angiogenesis. Dovitinib strongly binds to fibroblast growth factor receptor 3 (FGFR3) and inhibits its phosphorylation, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell death. In addition, this agent may inhibit other members of the RTK superfamily, including the vascular endothelial growth factor receptor; fibroblast growth factor receptor 1; platelet-derived growth factor receptor type 3; FMS-like tyrosine kinase 3; stem cell factor receptor (c-KIT); and colony-stimulating factor receptor 1; this may result in an additional reduction in cellular proliferation and angiogenesis, and the induction of tumor cell apoptosis. There are several ongoing Phase I/III clinical trials for dovitinib.
Status:
Investigational
Source:
INN:squalamine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Squalamine is a steroid-polyamine conjugate compound with broad-spectrum antimicrobial activity and anti-angiogenic activity. Squalamine selectively inhibits new blood vessel formation; this activity is thought to be mediated through inhibition of the sodium-hydrogen antiporter sodium-proton exchangers (specifically the NHE3 isoform) causing inhibition of hydrogen ion efflux from endothelial cells, with subsequent reduction of cellular proliferation. Studies in tumor-bearing mice have shown that squalamine inhibits angiogenesis and tumor growth in xenograft models of lung, breast, ovarian, and prostate cancer and in brain and breast allograft tumor models in rats. Squalamine also has been shown to prevent lung metastases in the murine Lewis lung carcinoma model, both as a single agent and in combination with various other chemotherapeutics. Squalamine does not appear to have substantial direct effects on primary tumor growth in animal models when administered as a single agent. However, enhanced antitumor responses are observed when squalamine is administered in combination with cytotoxic chemotherapeutic agents when compared with cytotoxic agents used alone. Squalamine was studied as a potential cancer drug and as a potential treatment for wet macular degeneration but as of 2018 had not succeeded in Phase III trials for any use.
Status:
Other

Class (Stereo):
CHEMICAL (RACEMIC)

Emoxypine (ethylmethylhydroxypyridine) succinate (MEXIDOL®) is a 3-hydroxypyridine derivative which is quite similar in structure to Vitamin B6 (pyridoxine). The most important components of the mechanism of action of Mexidol® are its antioxidant and membranotropic effects, the ability to modulate functioning of receptors and membrane-bound enzymes, restore a neurotransmitter balance. Due to its mechanism of action Mexidol® has a wide range of pharmacological effects, realized on at least two levels – neuronal and vascular. It has antihypoxic, anti-ischemic, neuroprotective, nootropic, vegetotrophic, anti-stress, anxiolytic, anticonvulsant, anti-alcohol, cardioprotective, anti-atherogenic, geroprotective and other actions. Under the action of Mexidol®, it is observed an improvement in cerebral circulation and microcirculation. Emoxypine is distributed in Russia but it is widely unknown in other regions.
Panobinostat is an oral deacetylace (DAC) inhibitor approved on February 23, 2015 by the FDA for the treatment of multiple myeloma. The approval was accelerated based on progression-free survival, therefore confirmatory trials by the sponsor to demonstrate clinical efficacy in multiple myeloma treatment are in progress of being conducted. Panobinostat is marketed by Novartis under the brand name Farydak. Panobinostat is a deacetylase (DAC) inhibitor. DACs, also known as histone DACs (HDAC), are responsible for regulating the acetylation of about 1750 proteins in the body; their functions are involved in many biological processes including DNA replication and repair, chromatin remodelling, transcription of genes, progression of the cell-cycle, protein degradation and cytoskeletal reorganization. In multiple myeloma, there is an overexpression of DAC proteins. Panobinostat inhibits class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10) and class IV (HDAC 11) proteins. Panobinostat's antitumor activity is believed to be attributed to epigenetic modulation of gene expression and inhibition of protein metabolism. Panobinostat also exhibits cytotoxic synergy with bortezomib, a proteasome inhibitor concurrently used in treatment of multiple myeloma.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Lactic acid, D- is a natural optical isomer of lactic acid. It is a poorly utilized isomer – 30 to 40% of the dose ingested is excreted in the urine. Lactic acid, D- is known to be harmful to human metabolism and it can result in acidosis and decalcification. D-lactic acidosis, also referred as D-lactate encephalopathy, has been reported in patients with short bowl syndrome. Lactic acid, D- is an interesting precursor for manufacturing heat-resistant polylactic acid (PLA) bioplastics which can be widely used, for example as packaging material, coatings, for textiles or in the automotive industry.
Status:
Possibly Marketed Outside US
Source:
Canada:SARCOLACTIC ACID
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Lactic Acid, L- (L-lactic acid, L-lactate) is the levorotatory isomer of lactic acid, the biologically active isoform in humans. Lactic acid or lactate is produced during fermentation from pyruvate by lactate dehydrogenase. Lactate dehydrogenase is isomer-specific so that production and metabolism of D-lactate require D-LDH and L-lactate requires L-LDH. Mammalian cells only contain L-LDH so that in humans the lactate produced is almost exclusively L-lactate. Carbohydrate-fermenting bacterial species (e.g. lactobacillus spp) have by contrast both enzymes and therefore the capacity to produce both D-lactate and L-lactate. L-lactic acid is the primary agonist of hydroxycarboxylic acid receptor 1 (HCA1), which is a Gi/o-coupled G protein-coupled receptor (GPCR). Poly-L-lactic acid is an absorbable, semi-permanent, injectable implant that can be used to restore volume and stimulate collagen formation gradually. It is FDA-approved for the correction of facial fat loss associated with antiretroviral therapy-induced lipoatrophy in HIV patients. It is FDA-approved for use in immunocompetent people for the correction of nasolabial fold deficiencies and other facial wrinkles. It has been used off-label to enhance the cheeks, hands, neck, thighs, gluteal enhancement and chest wall deformities, such as pectus excavatum or thoracic deformities secondary to surgical procedures.
Status:
Possibly Marketed Outside US
Source:
Amsa Pd Inj 50mg/ml by Erfa Canada 2012 Inc [Canada]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Aminoacridine derivative that is a potent intercalating antineoplastic agent. It is effective in the treatment of acute leukemias and malignant lymphomas, but has poor activity in the treatment of solid tumors. It is frequently used in combination with other antineoplastic agents in chemotherapy protocols. It produces consistent but acceptable myelosuppression and cardiotoxic effects. Although its mechanism of action is incompletely defined, amsacrine inhibits DNA synthesis by binding to and intercalating with DNA. Amsacrine also inhibits topoisomerase II activity and may exert an effect on cell membranes. This agent also possesses immunosuppressive and antiviral properties. While amsacrine is not cell cycle phase-specific, cytotoxicity is maximal during the G2 and S phases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Bamipine (trade name Soventol) is a sedating antihistamine with pronounced sedative effects. Bamipine is a pharmaceutical drug acting as an H1 antihistamine with anticholinergic properties. It is used as an antipruritic ointment. Bamipine hydrochloride has been given by mouth. Bamipine, bamipine lactate, and bamipine salicylate have all been applied topically.

Showing 41 - 50 of 52 results