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

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Showing 301 - 310 of 511 results

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:
NCT04359615: Phase 4 Interventional Unknown status COVID-19
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Favipiravir (originally known as T-705) is an orally administered novel anti-viral compound with a unique mechanism of action that is active against a wide range of RNA-based viruses in laboratory tests. Favipiravir has recently being approved in Japan under the brand name Avigan. Avigan is an experimental antiviral drug being developed by Toyama Chemical of Japan. It is a viral RNA polymerase inhibitor with a new mechanism of action, inhibiting viral gene replication within infected cells to prevent the propagation. Favipiravir is phosphoribosylated by cellular enzymes to its active form, favipiravir-ribofuranosyl-5′- triphosphate (RTP). Favipiravir is active against a broad range of influenza viruses, including A(H1N1)pdm09, A(H5N1) and the recently emerged A(H7N9) avian virus. It also inhibits influenza strains resistant to current antiviral drugs, and shows a synergistic effect in combination with oseltamivir, thereby expanding influenza treatment options. A Phase III clinical evaluation of favipiravir for influenza therapy has been completed in Japan and two Phase II studies have been completed in the United States. In addition to its anti-influenza activity, favipiravir blocks the replication of many other RNA viruses, including arenaviruses (Junin, Machupo and Pichinde); phleboviruses (Rift Valley fever, sandfly fever and Punta Toro); hantaviruses (Maporal, Dobrava, and Prospect Hill); flaviviruses (yellow fever and West Nile); enteroviruses (polio- and rhinoviruses); an alphavirus, Western equine encephalitis virus; a paramyxovirus, respiratory syncytial virus; and noroviruses.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Butanilicaine (Hostacain) is a local anesthetic. It uses may associate with a risk of allergy. Butanilicaine has a vasodilator effect.
Status:
Possibly Marketed Outside US
Source:
Japan:Miproxifene Phosphate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

TAT-59 (Miproxifene Phosphate) is a triphenylethylene analog of tamoxifen. TAT-59 is the phosphate ester prodrug of the practically insoluble parent drug DP-TAT-59. It is an antiestrogen developed in Japan for breast cancer. It is a potent antitumor agent for hormone-dependent tumors. Most of TAT-59 metabolites possessed remarkable binding affinity toward estrogenic receptors as well as fairly good antiuterotrophic activity.
Status:
Possibly Marketed Outside US
Source:
Japan:Cytarabine Ocfosphate
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cytarabine ocfosfate (commercial name: Starasid) is a prodrug having stearyl group attached to phosphoric acid at 5' position of arabinose moiety of cytosine arabinoside (Ara-C). This drug is given orally. The mode of action is in the inhibition of DNA synthesis after conversion to Ara-CTP as in Ara-C. The drug is metabolized in the liver, producing the intermediate metabolite, C-C3PCA which is converted to Ara-C gradually. This property results in the maintenance of relatively long time the blood Ara-C levels. This was proved to be active clinically against acute leukemia and MDS.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluoroethylcholine ion F-18 is ethylcholine labeled with fluorine F 18, a positron-emitting isotope. Fluorine F18 fluoroethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, and finally is integrated into cellular phospholipids, probably primarily into a phosphatidyl derivative; concentration of this agent in tumor cells as various fluorine F 18 fluoroethylcholine derivatives enables tumor imaging using positron emission tomography (PET). Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently up-regulated in human tumor cell lines. F18-fluoroethylcholine is used for imaging of prostate cancer and brain tumors, mainly in Europe and Japan.
Status:
Possibly Marketed Outside US
Source:
Unknown by Santhera Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pimasertib) (N-[(2S)-2,3-dihydroxypropyl]-3-[(2-fluoro-4-iodophenyl)amino]isonicotinamide hydrochloride; AS703026), a highly selective, potent, ATP non-competitive allosteric inhibitor of MEK1/2. It binds to MEK1/2 in an allosteric site that is distinct from, yet in close proximity to, the ATP binding site. Binding to this allosteric site prevents the activation of MEK1/2. Pimasertib continues to be investigated in patients with NRAS mutant malignant melanoma in a Phase II trial. This drug was discontinued in a combination with SAR245409 for Phase II study in low-grade serous ovarian cancer. This decision was based on the results of a futility analysis, conducted by the IDMC, which indicated that the trial was no longer expected to achieve its objective of showing a meaningful difference between the efficacies of the combination compared with pimasertib alone. The further development of pimasertib in pancreatic cancer was also discontinued, as a Phase II study in this indication did not reach its primary endpoint of prolongation of progression-free survival
Status:
Possibly Marketed Outside US
Source:
Canada:MYRISTAMIDOPROPYL DIMETHYLAMINE
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Myristamidopropyl dimethylamine [MAPD] is an amidoamine compound that shows activity against Acanthamoeba as well as a variety of other causal agents of microbial keratitis. MAPD, present in Opti-Free Express Multi-Purpose Disinfecting solution for contact lenses, has been shown to exhibit anti-acanthamoeba activity. Challenge test assays were used to study the efficacy of 50 mg/L MAPD against Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans, Fusarium solani and Acanthamoeba polyphaga. MAPD gave a 3.7 log kill of P. aeruginosa after 60 min, 5.4 log for S. aureus by 45 min and 5 log for C. albicans and F. solani within 15 min. A. polyphaga cysts were reduced by 4 log within 120 min. MAPD also possesses excellent antifungal and antibacterial activity. MAPD may represent a broad-spectrum therapeutic antimicrobial for keratitis and surgical prophylaxis and deserves further evaluation in these roles. Myristamidopropyl dimethylamine uses and applications also include: surfactant; emulsifier for cosmetics and toiletries; conditioner; viscous builder; softener for textile finishes.
Ligustrazine (tetramethylpyrazine) is a bioactive ingredient extracted from the widely-used Chinese herb, Chuanxiong. It inhibits of platelet aggregation, enhances of vessel dilation, increases cerebral blood flow and possesses neuroprotective properties. The injection solution of ligustrazine has been used especially in China to treat ischemic stroke, coronary heart disease, diabetic nephropathy, and knee osteoarthritis. Ligustrazine was also evaluated in clinical as a remedy for pressure sores, as a salvage agent for patients with non-Hodgkin's lymphoma, as a treatment for bronchial asthma and vertebrobasilar insufficiency.

Showing 301 - 310 of 511 results