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

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Showing 141 - 150 of 479 results

Status:
Possibly Marketed Outside US
Source:
NCT00994461: Phase 4 Interventional Completed Healthy Volunteers
(2009)
Source URL:

Class (Stereo):
CHEMICAL (MIXED)



Loxoprofen (INN) is a non-steroidal anti-inflammatory drug in the propionic acid derivatives group. It is marketed in Brazil, Mexico and Japan by Sankyo as its sodium salt, loxoprofen sodium, under the trade name Loxonin, Argentina as Oxeno and in India as Loxomac. It is available in these countries for oral administration, and a transdermal preparation was approved for sale in Japan on January 2006. It is usually used to treat rheumatoid arthritis and osteoarthritis. It is also used to reduce pain and inflammation after surgery, wounds and tooth removal, as well as to bring down fever or ease pain induced by acute inflammation of upper respiratory tract Loxoprofen is a prodrug. When administered orally, loxoprofen sodium hydrate is absorbed from the gastrointestinal tract as an unchanged compound with only a modest gastric-mucosal irritation. It is then rapidly biotransformed into the active metabolite trans-OH form (SRS coordination) with a potent inhibitory effect on prostaglandin biosynthesis to exert its pharmacologic effects. Inhibition of prostaglandin biosynthesis constitutes the mechanism of action of this drug, the site of action being cyclooxygenase.
Ergosterol was discovered over 100 years ago in the plant pathogenic ergot fungus Claviceps purpurea. Ergosterol is the major fungal membrane sterol that regulates membrane fluidity, plasma membrane biogenesis and function. Antifungal drugs such as Amphotericin B exerts its action by simply binding ergosterol. Vitamin D2 (ergocalciferol) is derived from ergosterol by UVB irradiation. Ergocalciferol is used for treating low parathyroid hormone levels, rickets (a vitamin D deficiency condition), and low phosphate levels in the body.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Dapivirine, an anti-retroviral (ARV)-based microbicide, is a substituted diaminopyrimidine (DAPY) derivative and a potent non-nucleoside reverse-transcriptase inhibitor (NNRTI) with antiviral activity against HIV-1. Dapivirine showed high activity against wild-type and mutant HIV in in virto HIV models inhibiting a broad panel of HIV-1 isolates from different classes, including a wide range of NNRTI-resistant isolates. Developed by Janssen Sciences (formerly Tibotec Pharmaceuticals), dapivirine was initially tested as an oral treatment for HIV in a number of Phase I/II clinical trials. In 2014 the International Partnership for Microbicides (IPM) began its work on the monthly dapivirine ring. Phase I/II clinical trials in Africa, Europe and the United States proved that dapivirine is safe and well-tolerated. Phase III long-term safety and efficacy studies of the monthly dapivirine ring as part of IPM's Dapivirine Ring Licensure Program confirmed that the monthly dapivirine ring can safely help prevent HIV infection in women. In 2016 the ASPIRE Study reported a 27 percent reduction in HIV-1 acquisition with a trend toward greater protection in women over age 21 and no significant protection for women under age 21.
Status:
Possibly Marketed Outside US
Source:
ACOFIDE by Zeria
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Acotiamide (Acofide(®)), an oral first-in-class prokinetic drug, is under global development by Zeria Pharmaceutical Co. Ltd and Astellas Pharma Inc. for the treatment of patients with functional dyspepsia. The drug modulates upper gastrointestinal motility to alleviate abdominal symptoms resulting from hypomotility and delayed gastric emptying. It exerts its activity in the stomach via muscarinic receptor inhibition, resulting in enhanced acetylcholine release and inhibition of acetylcholinesterase activity. Acofide® is launched in Japan for treating functional dyspepsia.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Flupirtine is a triaminopyridine derivative having a chemical structure - 2-amino-3-ethoxy-carbonylamino-6-4-fluoro-benzylamino-pyridine. The basic molecule used for synthesis of flupirtine was 2, 6-dichoro 3-nitropyridine. It was first synthesized in 1980s in Germany and was marketed by Degussa Pharma. Flupirtine is a centrally acting, non-opioid analgesic that is available in a number of European countries for the treatment of a variety of pain states. The therapeutic benefits seen with flupirtine relate to its unique pharmacological properties. Flupirtine displays indirect NDMA receptor antagonism via activation of potassium channels and is the first representative of a pharmacological class denoted the 'selective neuronal potassium channel openers'. The generation of the M-current is facilitated by flupirtine via the opening of neuronal Kv7 potassium channels. The opening of these channels inhibits exaggerated neuronal action potential generation and controls neuronal excitability. Neuronal hyperexcitability is a physiological component of many pain states such as chronic pain, migraine and neurogenic pain.
Ornidazole is nitroimidazole derivative. It is an antiprotozoal drug that has proven to be effective against Trichomonas vaginalis, Entoamoeba histolytica, Giardia lamblia and Helicobacter pylori. The reduction of the nitro group and the generation of short-lived reactive intermediates are the basis of its parasiticidal activity. Ornidazole is a DNA-tropic drug with selective activity against microorganisms with enzyme systems capable of reducing the nitrogroup and catalyze the interaction between ferrodoxin proteins and nitrocompounds. After the drug penetrates the microbial cell, the mechanism of its action is based reducing the nitrogroup under the influence of the microorganism’s nitroreductases and the activity of the reduced nitroimidazole. The reduction products create compounds with DNA causing it to degrade, and disrupt the DNA replication and transcription processes. Furthermore, the drug’s metabolism products have cytotoxic properties and disrupt cellular respiration processes. It is indicated for the treatment of anaerobic systemic infections caused by ornidazole-sensitive microflora, prevention of infections caused by anaerobic bacteria, during operative treatment (especially middle and straight intestine surgeries), gynecological surgeries, severe intestinal ameobiasis, all extra-intestinal ameobiasis forms, giardiasis. Ornidazole was shown to be effective for the prevention of recurrence of Crohn's disease after ileocolonic resection.
Status:
Possibly Marketed Outside US
Source:
Unknown
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Hymecromone (4-methylumbelliferone) is already approved drug in Europe and Asia where it is used to treat biliary spasm. It is used as choleretic and antispasmodic drugs and as a standard for the fluorometric determination of enzyme activity. The concomitant administration of Hymecromone with products, containing metoclopramide, leads to mutual decrease of their action. Due to a danger of diarrhea with subsequent hypokalemia, Hymecromone should be applied with caution to patients on cardiac glycosides therapy (in these cases the sensitivity to them is increased). Hymecromone can be administered simultaneously with otherspasmolytics and analgesics. Very rare allergic reactions, itching, erythema, rashes; diarrhea which normally disappears by reduction of dose or discontinuance of therapy.
Status:
Possibly Marketed Outside US
Source:
Dorixina by Schering
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Clonixin is a nonsteroidal agent. It is an anilino-nicotinic acid derivative. It is a drug of anti-inflammatory antipyretic and analgesic activity that produces minor digestive side-effects. At high concentrations, clonixin inhibited PGE2 formed by COX-2 and partly by COX-1 activity. The drug is indicated for the relief of headaches, muscle aches, joint, dental, ear, dysmenorrhea, post-traumatic, post-surgical, gynecological. Adverse effects are occasionally nausea, dizziness, and somnolence, were mild and transient. On rare occasions, and administering high doses, it is possible the appearance of dry mouth or constipation. Concomitant use of anticholinergic drugs to be avoided by the possibility that they enhance their effects atropine.
mixture
Status:
First approved in 2001

Class:
MIXTURE



Norelgestromin, the progestin, is the active metabolite of norgestimate and is structurally related to 19-nortestosterone. Norgestimate and norelgestromin mimic the physiologic effects of progesterone at the progesterone receptor. Johnson & Johnson developed an adhesive female contraceptive patch that contains ethinylestradiol (0.75mg) and the progestogen norelgestromin (6mg). his product is a combination contraceptive acting via the inhibition gonadotropins. Its primary mechanism of action involves the suppression of ovulation, including changes in the cervical mucus and endometrium. The patch delivers a continuous flow of hormones through the skin and into the bloodstream. The contraceptive patch is available in countries worldwide.
mixture
Status:
First approved in 1989

Class:
MIXTURE



Norgestimate is a steroidal progestin of the 19-nortestosterone group that is used in combination with ethinylestradiol as an oral contraceptive and for treatment of acne. and in combination with estradiol in menopausal hormone replacement therapy. Norgestimate shows high selectivity for the progesterone receptor and low androgenic activity.

Showing 141 - 150 of 479 results