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

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Showing 2951 - 2960 of 4697 results

Status:
Possibly Marketed Outside US
Source:
NCT02088515: Phase 4 Interventional Completed Squamous Cell Carcinoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Nedaplatin is a second-generation cisplatin analogue with antineoplastic activity. nedaplatin forms reactive platinum complexes that bind to nucelophillic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death. It is currently registered for the treatment of various cancers (head and neck, testicular, lung, ovarian, cervical, non-small-cell lung) in Japan. The most commonly reported adverse reactions include nausea, vomiting, loss of appetite and hair loss. Nedaplatin may also cause nephrotoxicity at therapeutic doses, especially in patients with deteriorating renal function.
Status:
Possibly Marketed Outside US
Source:
CALSED by Sumitomo Pharmaceuticals
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Amrubicin is a totally synthetic 9-aminoanthracycline anticancer drug, which is approved in Japan for the treatment of small cell and non-small cell lung cancer. Upon administration amrubicin is reduced to its C-13 hydroxy metabolite, amrubicinol. The cytotoxicity of amrubicinol in vitro is 10 to 100 times greater than that of amrubicin. Thus, the anticancer activity of amrubicin is considered to derive from this active metabolite. The mechanism of action of the drug is related to the inhibition of topoisomerase II by stabilizing the cleavable complex.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Vosaroxin is a small molecule and a naphthyridine analogue with antineoplastic activity. This quinolone-based topoisomerase II inhibitor is a new therapeutic for acute myeloid leukemia (AML). Being a DNA intercalating topoisomerase II inhibitor that causes the induction of apoptosis via double-strand DNA breaks vosoroxin is chemically distinct from other topoisomerase inhibitors with its stable quinolone-based core. Due to the stability of this core, vosaroxin is not associated with significant formation of toxic metabolites, free radicals, or reactive oxygen species, which are associated with off-target organ damage and cardiotoxicity. Furthermore, vosaroxin evades two common mechanisms of drug resistance, as it is not a substrate for the P-glycoprotein efflux pump and its activity is maintained in cells with p53 deletion. Vosaroxin has beeт tested in several investigator-sponsored studies, both as a single-agent and in combination with other therapies, for the treatment of AML and myelodysplastic syndromes. Both the U.S. Food and Drug Administration (FDA) and European Commission have granted orphan drug designation to vosaroxin for the treatment of AML. Additionally, vosaroxin has been granted fast track designation by the FDA for the potential treatment of relapsed or refractory AML in combination with cytarabine. Vosaroxin is an investigational drug that has not been approved for use in any jurisdiction. The trademark name QINPREZO is conditionally accepted by the FDA and the EMA as the proprietary name for the vosaroxin drug product candidate.
Status:
Possibly Marketed Outside US
Source:
Japan:Epristeride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Epristeride is a steroid 5-alpha-reductase inhibitor developed for the treatment of prostatic hyperplasia and acne. The drug reached phase III clinical trial for hyperplasia in the UK, the US and Japan, however, the current status of the drug is unknown.
Status:
Possibly Marketed Outside US
Source:
NCT02478242: Phase 4 Interventional Completed Acute Kidney Injury
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Nafamostat mesilate (NM), a synthetic serine protease inhibitor, has anticoagulant and anti-inflammatory properties. Nafamostat is approved and marketed in Japan. It relieves symptoms such as pain due to inflammation of the spleen. It improves visceral disorders and bleeding tendency caused by blood clotting tendency in the vessels. It prevents coagulation in the blood circuit during hemodialysis. It is usually used to improve acute symptoms of pancreatitis (acute pancreatitis, acute exacerbation phase of chronic pancreatitis, post-operative acute pancreatitis, acute pancreatitis after pancreatography, traumatic pancreatitis) and to prevent disseminated intravascular coagulation (DIC) and clotting of perfusing blood in extracorporeal blood circuit. Nafamostat mesilate significantly inhibits the release of platelet beta-thromboglobulin (beta TG) at 60 and 120 min. Nafamostat mesilate (NM) prevents any significant release of neutrophil elastase; at 120 min, plasma elastase-alpha 1-antitrypsin complex is 0.16 mg/mL in the NM group and 1.24 mg/mL in the control group. Nafamostat mesilate completely inhibits formation of complexes of C1 inhibitor with kallikrein and FXIIa.
Status:
Possibly Marketed Outside US
Source:
Japan:Spiperone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class. Spiperone is selective D2 dopamine receptor antagonist; α1B-adrenoceptor antagonist; mixed 5-HT2A/5-HT1 serotonin receptor antagonist. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis. Spiperone is widely used as a pharmacological tool for studying neurotransmitter receptors.
Status:
Possibly Marketed Outside US
Source:
NCT04479813: Phase 4 Interventional Completed Central Sympathetic Nervous System Diseases
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Moxonidine is a second-generation, centrally acting antihypertensive drug with a distinctive mode of action. Moxonidine activates I1-imidazoline receptors (I1-receptors). Imidazoline I1-receptor agonism represents a new mode of antihypertensive action to inhibit peripheral alpha-adrenergic tone by a central mechanism. Adrenaline, noradrenaline and renin levels are reduced, a finding consistent with central inhibition of sympathetic tone. Moxonidine acts centrally to reduce peripheral sympathetic activity, thus decreasing peripheral vascular resistance. In patients with mild to moderate hypertension, moxonidine reduces blood pressure (BP) as effectively as most first-line antihypertensives when used as monotherapy and is also an effective adjunctive therapy in combination with other antihypertensive agents. It improves the metabolic profile in patients with hypertension and diabetes mellitus or impaired glucose tolerance, is well tolerated, has a low potential for drug interactions and may be administered once daily in most patients. Moxonidine is a good option in the treatment of patients with mild to moderate hypertension, particularly as adjunctive therapy in patients with the metabolic syndrome.
Status:
Possibly Marketed Outside US
Source:
NCT01661985: Phase 4 Interventional Unknown status Urethritis
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lymecycline is a tetracycline broad-spectrum antibiotic marketed by the pharmaceutical company Galderma. It is approximately 5,000 times more soluble than tetracycline base and is unique amongst tetracyclines in that it is absorbed by an active transport process across the intestinal wall, making use of the same fast and efficient mechanism by which carbohydrates are absorbed. Lymecycline's side effects can include rash, headache, diarrhoea, ulcerative colitis, nausea, vomiting, dermatitis, dysphasia, inflammation of the liver, hypersensitive reactions, and visual disturbances. When taken for a long period of time, it can cause reflux oesophagitis.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)


Calmatel contains piketoprofen and belongs to the group of drugs called nonsteroidal anti-inflammatory drugs (NSAIDs). This medicine is indicated in adolescents over 12 years and adults for local pain relief and mild and occasional inflammation caused by: small contusions, bruises, strains; torticollis or other contractures; lumbago; minor sprains caused because of a twist.
Status:
Possibly Marketed Outside US
Source:
NCT03077555: Phase 4 Interventional Completed Ovulation Inhibition
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nomegestrol acetate (NOMAC) is a 19-norprogesterone derivative with high biological activity at the progesterone receptor, a weak anti-androgenic effect, but with no binding to estrogen, glucocorticoid or mineralocorticoid receptors. Nomegestrol has been developed by the Monaco-based company Théramex SAM (a Teva subsidiary). Nomegestrol acetate has been used successfully for the treatment of some gynaecological disorders (menstrual disturbances, dysmenorrhoea, premenstrual syndrome) and as a component of hormone replacement therapy in combination with estradiol for the relief of menopausal symptoms; it has been approved in Europe as monotherapy for the treatment of the menopausal syndrome, uterine diseases and menorrhagia, and in combination with an estrogen for the treatment of menopausal symptoms. Nomegestrol acetate in combination with estradiol is used as an oral contraceptive.

Showing 2951 - 2960 of 4697 results