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

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Showing 121 - 130 of 188 results

Lysing is an essential basic amino-acid encoded by codone AAA and AAG, and used in the biosynthesis of proteins. The daily requirement for lysine is 38 mg/kg body weight. The most rich source of lysine is fish, beef, chicken. In a clinical study lysine supplements was found to be an effective for reduction of occurrence, severity and healing time for recurrent HSV infection, however Cochrane Review concluded that the evidence is insufficient. Lysine was investigated for improving anxiety, ameliorating angina prectoris. Lysine acetylsalicylate has been used to treat pain and to detoxify the body after heroin use. Lysine clonixinate has been used for its analgesic properties for the treatment of migraine headaches and other painful conditions. However, limited clinical trials exist for these conditions.
Status:
US Previously Marketed
First approved in 1961

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tyrosine (L-form) is a non-essential amino acid, which is primarily required for the protein synthesis. This amino acid is the precursor of dopamine, norepinephrine, and epinephrine; therefore the lower concentration of tyrosine could be a peripheral marker of the hyperdopaminergic condition hypothesized to explain psychosis. Tyrosine supplements can improve cognition, increase energy, reduce anxiety, reduce depression, reduce levels of pain.
N-Acetyltyrosine is an acetylated derivative of the amino acid L-tyrosine. Ordinary L-tyrosine is less stable and also less soluble in water, which may result in reduced bioavailability. Acetylation enhances the solubility and stability of certain amino acids. N-Acetyltyrosine is commonly used in place of tyrosine in parenteral nutrition. It converts to tyrosine and then can be used in neurotransmitter treatment as a precursor of cathecholamine. N-Acetyltyrosine supports brain function by supporting the synthesis of the catecholamines norepinephrine and dopamine (neurotransmitters). N-Acetyltyrosine supplements are used to improve memory and cognitive performance in humans while they are experiencing psychological stress.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Cediranib (AZD-2171) is a VEGFR-2 kinase inhibitor which was developed by AstraZeneca for the treatment of cancer. The drug reached the final stage of approval by European Medicines Agency in 2008 under the name Zemfirza (it was recommended to be taken in combination with platinum-based chemotherapy), however on 19 September 2016 AstraZeneca decided to withdraw the Marketing Authorisation Application.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Olmutinib is a novel third-generation epidermal growth factor receptor (EGFR) mutation-specific tyrosine kinase inhibitor, used in the treatment of T790M mutation positive non-small cell lung cancer. Olmutinib covalently binds a cysteine residue near the kinase domain of mutant EGFRs to prevent phosphorylation of the receptor. EGFRs are frequently over-expressed in lung cancer and contribute to activation of the phosphoinositide 3-kinase and mitogen-activated protein kinase pathways which both promote cell survival and proliferation. By inhibiting EGFR activation, Olmutinib attenuates the activation of these tumor-promoting pathways. In the first phase I/II clinical study of Osimertinib, 800 mg/ day was chosen as the dose for subsequent studies, and the dose-limiting toxicity and maximum tolerated dose was not reached. Olmutinib received breakthrough therapy designation in the United States in December 2015 and was approved for use in Korea in May 2016.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

18F-FET (18F-Fluoroethyl-L-tyrosine) is a radiolabelled amino acid. It penetrates the blood-brain barrier by a specific amino acid transport system. In the brain, it is taken up into upregulated tumoral cells but not incorporated into proteins. It is used as a biomarker for positron emission tomography for imaging brain tumors, where it has higher specificity than 18F-FDG.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Rociletinib is a novel, potent, small molecule, third generation TKI that irreversibly binds and inhibits EGFR with the common activating (L858R, Del19) and T790M resistance mutations. The proposed indication of rociletinib is for the treatment of patients with mutant EGFR NSCLC who have been previously treated with an EGFR-targeted therapy and have the T790M mutation as detected by an FDA approved test. The results from two Phase 2 studies show that rociletinib 625 mg BID treatment has a favorable benefit:risk profile in patients with recurrent T790M-positive mutant EGFR NSCLC based on clinically meaningful and durable responses and a well-established and acceptable safety profile in this patient population with terminal lung cancer. In May 2016, Clovis Oncology, Inc. announced it has terminated enrollment in all ongoing sponsored studies of rociletinib, including TIGER-3, after the company was notified at meeting with the FDA that it could anticipate receiving a Complete Response Letter (CRL) for the rociletinib NDA on or before the PDUFA date of June 28, 2016. Clovis has also withdrawn its Marketing Authorization Application of rociletinib with European regulatory authorities.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dibromotyrosine is a brominated derivative of a natural amino acid tyrosine. In the human body, dibromotyrosine is produced by eosinophil peroxidase secreted from activated eosinophils. Dibromotyrosine is naturally produced by marine sponges. Dibromotyrosine is used in medicine for the treatment of functional hyperthyroidisms. It acts by competing with iodination of tyrosines, thus reducing the active form of the thyroid hormones. Dibromotyrosine also appears to maintain the ability to control TSH production through negative feedback on the pituitary gland, reducing the biological activity of the thyroid. Dibromotyrosine is marketed in Italy under tradename Bromotiren.

Showing 121 - 130 of 188 results