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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 321 - 330 of 1040 results

Lysophosphatidic acid (LPA) is a multifunctional intercellular phospholipid messenger. LPA stimulates the growth of a variety of cells including fibroblasts, vascular smooth muscle cells, endothelial cells, and keratinocytes. It is produced in relatively high levels from activated platelets and can be detected in bodily fluids including serum, saliva, follicular fluid, and malignant effusions. LPA acts as a proliferative and anti-apoptotic factor and is a ligand for LPA1 (EDG-2), LPA2 (EDG-4) and LPA3 (EDG-7) receptors. The plasma LPA level can be a useful marker for ovarian cancer, particularly in the early stages of the disease. It is known, that the therapeutic administration of LPA also blocked APAP-induced liver damage, leading to an increased survival rate by increasing the glutathione level but decreasing inflammatory cytokines in an LPA1,3,5-independent manner. Thus, LPA might be an important therapeutic agent for drug-induced liver injury. In addition, was shown, that LPA levels in plasma and ascites may be useful diagnostic biomarkers for peritoneal carcinomatosis of gastric cancer.
Status:
Possibly Marketed Outside US
Source:
Canada:URIC ACID
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Uric acid, generated from the metabolism of purines, has proven and emerging roles in human disease. Humans produce large quantities of uric acid. Excess serum accumulation of uric acid can lead to a type of arthritis known as gout. Hyperuricemia may increase risk factors for cardiovascular disease. High serum uric acid was associated with higher risk of type 2 diabetes and other diseases.
Status:
Possibly Marketed Outside US
Source:
Dr. Cellapy SR Premium Solution by GM Holdings Co., Ltd
(2014)
Source URL:
First approved in 2014
Source:
Dr. Cellapy SR Premium Solution by GM Holdings Co., Ltd
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Cytosine is a pyrimidine nucleobase, one of the five main bases of nucleic acids. In DNA and RNA cytosine is paired with guanine. Only small amounts of cytosine administered with food are incorporated in DNA. The majority of cytosine is synthesized de-novo starting from carbamoyl phosphate.
Tetraxetan (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (also known as DOTA) is used as a complexing agent. Its complexes have medical applications as contrast agents and cancer treatments. DOTA can be conjugated to monoclonal antibodies by attachment of one of the four-carboxyl groups as an amide. The modified antibody accumulates in the tumour cells, concentrating the effects of the radioactivity of 90Y. DOTA can also be linked to molecules that have an affinity for various structures. The resulting compounds are used with a number of radioisotopes in cancer therapy and diagnosis. Clivatuzumab tetraxetan is a humanized monoclonal antibody targeting a mucin antigen expressed in most pancreatic cancers, but not pancreatitis, normal pancreas or most other normal tissues. Preclinical studies in mice with human pancreatic cancer xenografts given the murine version of 90Y-clivatuzumab tetraxetan demonstrated favourable tumour responses, which could be further improved when given in combination with gemcitabine. (64)Cu-DOTA-trastuzumab PET (positron emission tomography) could be a potential noninvasive procedure for serial identification of metastatic brain lesions in patients with HER2-positive breast cancer. 90Y-DOTA-biotin may have the application of pre-targeted radioimmunotherapy for the treatment of advanced colorectal cancer in humans.
Technetium (99mTc) exametazime is a radiopharmaceutical agent, which is known as trade name Ceretec. The Ceretec kit is supplied as five packs of three vials for use in the preparation of a technetium Tc99m exametazime intravenous injection as a diagnostic radiopharmaceutical. When technetium Tc99m pertechnetate is added to exametazime in the presence of stannous reductant, a lipophilic technetium Tc99m complex is formed. This lipophilic complex is the active moiety. It converts at approximately 12%/hour to less lipophilic species. When the secondary complex is separated from the lipophilic species, it is unable to cross the blood-brain-barrier. The useful life of the reconstituted agent is limited to 30 minutes. This complex is used as an adjunct in the detection of altered regional cerebral perfusion in stroke. And in addition, is indicated for leukocyte labeled scintigraphy as an adjunct in the localization of intra-abdominal infection and inflammatory bowel disease. Also exist clinical trials, where this complex is used for diagnostic purposes in Crohn's Disease and in vascular prosthesis infection.
Status:
Possibly Marketed Outside US
Source:
NCT02140073: Phase 4 Interventional Unknown status GERD
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Domperidone is a peripherally selective D2 receptor antagonist. It acts as an antiemetic and a prokinetic agent through its effects on the chemoreceptor trigger zone and motor function of the stomach and small intestine. Domperidone was not approved in USA due to risks of cardiac arrhythmias, cardiac arrest, and sudden death, but is available in other countries. However, FDA allows access to Domperidone through an expanded access investigational new drug application (IND) to patients with gastroesophageal reflux disease with upper GI symptoms, gastroparesis, and chronic constipation. As an “off-label” use, domperidone is prescribed to breastfeeding women to enhance their milk production.
Status:
Possibly Marketed Outside US
Source:
NCT01904396: Phase 4 Interventional Unknown status Carnitine Deficiency
(2013)
Source URL:
First approved in 2009

Class (Stereo):
CHEMICAL (RACEMIC)

Conditions:

L-carnitine (L-beta-hydroxy-gamma-N,N,N-trimethylaminobutyric acid) is conditionally necessary for mitochondrial transport and metabolism of long-chain fatty acids, and thus for myocardial energetic metabolism. D-carnitine is not biologically active and might interfere with proper utilization of the L isomer, and so there are claims that the racemic mixture (DL-carnitine) should be avoided. The pharmacological effects of carnitine are stereospecific: L-carnitine was effective in various animal and clinical studies, while D- and DL-carnitine was found to be ineffective or even toxic to some cells and tissues, such as muscle cells and the myocardium. DL-carnitine caused symptoms of myasthenia and cardiac arrhythmias, which disappeared after L-carnitine administration.
Status:
Possibly Marketed Outside US
Source:
PROFENDER by Astellas Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Emodepside is a semi-synthetic product (originated by Astellas and out-licensed to Bayer for animal and human use); its precursor is synthesized by a fungus living in the leaves of Camellia japonica. It is a potent antihelminthic drug used in combination with praziquantel (as Profender®) and in combination with toltrazuril (as Procox®) for the treatment of parasitic worms in cats and dogs. Emodepside, a semi-synthetic derivative of PF1022A, belongs to a new class of anthelmintic drugs, the cyclooctadepsipeptides, and shows good efficacy against macrocyclic lactone-, levamisole- or benzimidazole-resistant nematode populations. Although putative receptors for emodepside have already been discovered, its mode of action is still not fully understood. It has being suggested that GABA(A)-receptor UNC-49 is associated with the emodepside mode of action. It has also being shown that Emodepside binds to a presynaptic latrophilin receptor in nematodes. The following presynaptic signal transduction occurs via activation of Gqalpha protein and phospholipase-Cbeta, which leads to mobilization of diacylglycerol (DAG). DAG then activates UNC-13 and synaptobrevin, two proteins which play an important role in presynaptic vesicle-functioning. This finally leads to the release of a currently unidentified transmitter. The transmitter (or modulator) exerts its effects at the postsynaptic membrane and induces a flaccid paralysis of the pharynx and the somatic musculature in nematodes.
Status:
Possibly Marketed Outside US
Source:
Advantage® DUO by Nihon Tokushu Noyaku Seizo K. K.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Imidacloprid is a systemic, chloro-nicotinyl insecticide used for the control of sucking insects such as fleas, aphids, whiteflies, termites, turf insects, soil insects, and some beetles. It is used on co on and vegetable crops as foliar and seed treatments, soil, structures, indoor and outdoor insect control, home gardening and pet products. It is indicated for the prevention of heartworm disease caused by Dirofilaria immitis. It kills adult fleas and is indicated for the treatment of flea infestations (Ctenocephalides felis). It is also indicated for the treatment and control of the following intestinal parasites Hookworm species, Roundworm species, Whipworms. Adverse events in animals included: malaise, vomiting, diarrhea, shaking, mydriasis, hypersalivation with abnormal neurologic signs, seizures, death, generalized hematoma of the body, and alopecia at the treatment site. Adverse reactions in humans included: burning, tingling, numbness, bad taste in the mouth, dizziness, and headache.
Status:
Possibly Marketed Outside US
Source:
Dectomax by Pfizer
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Doramectin is a macrocyclic lactone isolated from fermentations of selected strains derived from the soil organism Streptomyces avermitilis. A primary mode of action of macrocyclic lactones is to modulate chloride ion channel activity in the nervous system of nematodes and arthropods. Macrocyclic lactones bind to receptors that increase membrane permeability to chloride ions. This inhibits the electrical activity of nerve cells in nematodes and muscle cells in arthropods and causes paralysis and death of the parasites. Doramectin is indicated for the treatment and control of gastrointestinal roundworms, lungworms, eyeworms, grubs, biting and sucking lice, horn flies, and mange mites in cattle.