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

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Showing 2331 - 2340 of 8583 results

Pixantrone is a novel anthracenedione. It is a weak inhibitor of topoisomerase II. Pixantrone directly alkylates DNA forming stable DNA adducts and cross-strand breaks. Pixuvri is approved for the treatment of adult patients with multiply relapsed or refractory aggressive Non-Hodgkin lymphomas. It is used for patients whose cancer does not respond or has returned after they have received other chemotherapy treatments. The most frequent AE were seen in the blood (mainly neutropaenia), gastrointestinal (nausea, abdominal pain, constipation) and respiratory systems (cough, dyspnea). No drug-drug interaction studies have been submitted and no drug interactions have been reported in human subjects
Status:
Possibly Marketed Outside US
Source:
NCT01960192: Phase 4 Interventional Unknown status Primary CNS Lymphoma (PCNSL)
(2012)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Targets:


Fotemustine is a novel chloroethylnitrosourea alkylating agent approved for use in the treatment of metastasizing melanoma and Recurrent Malignant Gliomas. The antitumor activity of fotemustine is related to its ability to alkylate DNA. It's in vitro or in vivo pharmacological activity is similar or greater than that of other nitrosoureas. Significant activity has been found in mice xenograft models of human primary cerebral tumors after fotemustine intraperitoneal administration. Fotemustine has been registered for use in two indications: disseminated malignant melanoma, including cerebral metastases, and primary brain tumors. Fotemustine is currently used in Europe, particularly in France and Italy, as a salvage therapy for recurrent malignant gliomas. Myelosuppression, leucopenia, and thrombocytopenia are the most frequent side effects of treatment with fotemustine. The objective response to this treatment is between 26% and 70%, and the reported median survival time is 10 months. New drug combinations containing fotemustine and angiogenesis inhibitors, such as bevacizumab, are currently under development.
Status:
Possibly Marketed Outside US
Source:
SOLIMIDIN by Selvi & C Lab Bioterapico
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Zolimidine, a derivate of imidazopyridine, has a gastroprotective effect. It is used in the treatment of peptic ulcer and gastro-oesophageal reflux disease.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Formestane (trade name Lentaron) is a type I, steroidal, selective aromatase inhibitor used in the treatment of estrogen receptor-positive breast cancer in postmenopausal women. Formestane has poor oral bioavailability and thus must be administered fortnightly (bi-weekly) by intramuscular injection. Formestane is a second generation, irreversible, steroidal aromatase inhibitor. It inhibits the aromatase enzyme responsible for converting androgens to estrogens, thereby preventing estrogen production. Estrogen-sensitive breast cancer cells depend on estrogen for viability. Thus removal of estrogen from the body can be an effective treatment for hormone-sensitive breast cancers. Common side effects associated with the use of an aromatase inhibitor include hot flashes, joint pain, weakness, fatigue, mood changes, depression, high blood pressure, swelling of the arms/legs, and headache. Aromatase inhibitors may also decrease bone mineral density, which may lead to osteoporosis and an increase in fractures in susceptible patients. Formestane was the first selective aromatase inhibitor to be developed as a prescription drug, first appearing in Europe during the mid-1990s under the Lentaron Depot brand name. With the emergence of newer and more effective aromatase inhibitors, however, formestane soon lost market presence at a rapid rate. Most of the initial Lentaron preparations have since been discontinued. Currently, formestane (categorized as an anti-estrogenic agent) is prohibited from use in sports in accordance with the regulations of the World Anti-Doping Agency. The drug remains available today, but only in a small number of nations. This includes Austria, Brazil, Czech Republic, Hong Kong, and Turkey.
Status:
Possibly Marketed Outside US
Source:
CURATODERM by Teijin Pharma
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Talcalcitol is a synthetic analogue of vitamin D3. Tacalcitol has been developed by Teijin in Japan with the aim of maintaining the potent cell-regulating properties of calcitriol without the calcium-related adverse effects. Tacalcitol differs structurally from calcitriol by hydroxylation in the 24 position instead of the 25 position. Tacalcitol can influence the principal pathogenetic factors of psoriasis by inducing normalisation of keratinocyte differentiation, performing an anti-proliferative action and finally modulating the inflammatory response. Tacalcitol has been launched as an ointment formulation for the treatment of psoriasis in various countries. High-dose formulations (ointment and lotion) are available in Japan.
Status:
Possibly Marketed Outside US
Source:
Homoclomin by Eisai
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Homochlorcyclizine (INN) is an antihistamine which has been marketed in Japan since 1965. It is used in the treatment of Itching sensation resulting from skin diseases (eczema or dermatitis, pruritus, drug eruption, toxic erythema and infant strophulus), urticaria and allergic rhinitis. Homochlorcyclizine hydrochloride possesses several pharmacological properties: 1) inhibits bradykinin-induced contractions of isolated guinea pig ileum; 2)partially blocks SRS-A (slow-reacting substance of anaphylaxis )- induced contractions in isolated guinea pig il eum. 3) Homochlorcyclizine hydrochloride completely inhibits histamine-induced contractions at a concentration of 0.1μg/mL, while it completely inhibits serotonin or acetylcholine- induced contractions at a concentration of 1μg/mL.
Status:
Possibly Marketed Outside US
Source:
Oxyfedrine by Chemiewerk Homburg
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Oxyfedrine, an amino ketone derivative and partial agonist at beta receptors, has been shown to have potent antianginal properties and to increase coronary blood flow in normal and ischemic myocardial regions.
Status:
Possibly Marketed Outside US
Source:
Urelim by Gilman, H.|Arntzen, C.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Etebenecid is a uricosuric agent, lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys, also inhibits penicillin tubular secretion. It is useful in the interval treatment of gout. As with other uricosuric drugs, etebenecid may provoke acute gouty attacks in the early stages of treatment, and colchicine should be given during the first 6 weeks of treatment. It caused dyspepsia and diarrhea less frequently than probenecid and sulphinpyrazone. Several patients reported drowsiness while taking etebenecid in the treatment of gout, but no other side-effects were noted. Etebenecid should be given with care to patients with a history of uric acid calculi or of renal colic.
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
Source:
NCT00419796: Phase 4 Interventional Completed Osteoarthritis With Controlled Hypertension
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lumiracoxib is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug. On August 11, 2007, Australia's Therapeutic Goods Administration (TGA, the Australian equivalent of the FDA) cancelled the registration of lumiracoxib in Australia due to concerns that it may cause liver failure. New Zealand and Canada have also followed suit in recalling the drug. It has never been approved for use in the United States. Lumiracoxib has a different structure from the standard COX-2 inhibitors (e.g. celecoxib). It more closely resembles the structure of diclofenac (one chlorine substituted by fluorine, the phenylacetic acid has another methyl group in meta position), making it a member of the arylalkanoic acid family of NSAIDs. It binds to a different site on the COX-2 receptor than the standard COX-2 inhibitors. It displays extremely high COX-2 selectivity. The mechanism of action of lumiracoxib is due to inhibition of prostaglandin synthesis via inhibition of cyclooygenase-2 (COX-2). Lumiracoxib does not inhibit COX-1 at therapeutic concentrations. Lumiracoxib is used for the acute and chronic treatment of the signs and symptoms of osteoarthritis of the knee in adults.

Showing 2331 - 2340 of 8583 results