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Restrict the search for
megestrol acetate
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Status:
Investigational
Source:
INN:budiodarone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Budiodarone is a chemical analog of amiodarone with mixed ion channel electrophysiological activity. Budiodarone was developed to capitalize on the proven efficacy of amiodarone and to avoid its side effects. Budiodarone has a short plasma half-life (7 h) and a lower volume of distribution (13 L/kg). It is cleared from the body in 48 h. Like amiodarone, Budiodarone has balanced, multiple cardiac ion channel inhibiting activity, giving it properties of all four Vaughan Williams antiarrhythmic drug classes. Budiodarone, unlike amiodarone, undergoes rapid metabolism by plasma and tissue esterases. In clinical trials, Budiodarone effectively reduces the number and duration of atrial tachycardia/atrial fibrillation episodes.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Edifolone (SC-35135) is a structurally unique class Ia antiarrhythmic agent. It acts as a sodium channel antagonist. Edifolone development has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rifametane (SPA-S-565) is a semisynthetic derivative of rifamycin (a natural antibiotic produced by Amycolatopsis rifamycinica). It was being evaluated for treatment of bacterial infections. A phase I study showed that administration of rifametane is safe with minor, reversible adverse events such as mild headache, metallic taste and slightly elevated temperature for 3 to 4 hours. Rifametane has anti-tuberculosis activity and was suggested to be a good candidate for phase II clinical trials.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Siratiazem [LRA 113] is a calcium channel antagonist that is structurally similar to diltiazem but has a branched alkyl group on the basic nitrogen. Siratiazem has been developed in an attempt to limit the in vivo N-demethylation that is known to occur with diltiazem. Preliminary binding and functional studies in cardiac and vascular tissues indicate that it not only binds to diltiazem binding sites but also exhibits Ca2+ channel blocking
properties comparable to diltiazem. Siratiazem has a similar profile of activity to its parent compound, diltiazem, in that it blocks calcium channels in vascular, intestinal smooth muscle and cardiac tissue, and is least potent in cardiac muscle. At higher concentrations, siratiazem may also block cardiac sodium channels.
Class (Stereo):
CHEMICAL (ACHIRAL)
Brovanexine is a derivative of bromhexine used as an adjunct to antibacterials in preparations for the treatment of respiratory-tract infections. Oral administration of brovanexine hydrochloride (BR-222) caused a significant increase in the output volume of respiratory tract fluid. Brovanexine at 10 and 20 mg/kg showed a tendency to reduce the viscosity of respiratory tract fluid in anesthetized dogs. Brovanexine also showed a tendency to reduce the viscosity of sputum obtained from the SO2-exposed rabbits.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Ametantrone (AM) is a synthetic 9,10-anthracenedione bearing two (hydroxyethylamino)ethylamino residues at positions 1 and 4; along with other anthraquinones and anthracyclines, it shares a polycyclic intercalating moiety and charged side chains that stabilize DNA binding. Ametantrone is anticancer drug candidate targeting DNA. Ametantrone is a topoisomerase II inhibitor of the anthrapyrazole family. Ametantrone induces interstrand DNA cross-links in HeLa S3 cells. These cross-links were observed only in cellular system suggesting that metabolism of the drugs is a necessary step leading to DNA cross-linking. Ametantrone appeared to be very well tolerated and easy to handle. A dose-schedule of 135 mg/m2 q 2–3 weeks was recommended for phase II studies in solid tumors.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levonantradol is a synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) administered intramuscularly. It has antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2. Antiemetic effect of levonantradol significantly superior to chlorpromazine. However, its adverse central effects limit its utility. The main adverse events are drowsiness and dizziness. Levonantradol, administered intramuscularly to the patients suffering from postoperative pain, manifested significant analgesic efficacy. Analgesia persisted for more than 6 h with the 2.5 and 3 mg doses of levonantradol. Drowsiness was frequent but few other psychoactive effects were reported.
Class (Stereo):
CHEMICAL (ACHIRAL)
BROTIANIDE is salicylanilide derivative used to treat fascioliasis in sheep. A dose of 7 mg/kg of brotianide shows 91-99% activity against 7-14 weeks old flukes; however, its activity against 6 weeks old flukes is weak (50-90%). It also possesses 85-90% activity against paramphistomes in sheep and cattle. The maximum tolerated dose of brotianide is 27 mg/kg in sheep.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ozarelix is a luteinizing hormone-releasing hormone (LHRH) antagonist. It is known that LHRH antagonist exerts rapid inhibition of luteinizing hormone and follicle stimulating hormone with an accompanying rapid decrease in sex hormones. Thus this inhibitor can be effective in a variety of hormonally dependent disease including prostate cancer, benign prostatic hyperplasia (BPH), and endometriosis. Ozarelix was developed for the treatment of all these diseases including Alzheimer's disease. However, in January 2010 Spectrum Pharmaceuticals announced that it was discontinuing development of ozarelix in BPH. Because the low-dose intermittent therapy was disappointing in the treatment of lower urinary tract symptoms in men with BPH. The development of the drug for Alzheimer's disease was also discontinued. Ozarelix completed phase II trials for the treatment of prostate cancer and is in preclinical trials for the treatment of endometriosis and ovarian cancer.
Class (Stereo):
CHEMICAL (EPIMERIC)
Tropodifene (Tropaphen) is an α-Adrenergic receptor blocking agent. Clinical trials have shown that tropaphen has a beneficial effect on hypertension. Tropaphen has a very marked adrenolytic and vasodilator action. It greatly lowers the tone of the peripheral vessels. The preparation is effective starting with a dose of 0.1 mg/kg. After injection of the drug in a dose of 0.25 mg/kg, a considerable and gradually progressive decrease in the perfusion pressure takes place. The pressure falls by 30-35% and remained at a low level for 90-100 min. With a dose of tropaphen of 0.5 mg/kg, the perfusion pressure falls by 40-45% and remains low for 120 min or more. Strong vasodilatation is also observed after injection of tropaphen into intact rabbits.
