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

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Showing 141 - 150 of 194 results

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)



Fenticonazole is an imidazole derivative with a broad spectrum of antimycotic activity. It is used as a nitrate salt under different trade names (Lomexin, Gynoxin, Fentizol, etc) for the treatment of vaginal candidiasis. Fenticonazole inhibits the synthesis of ergosterol, an important step in the formation of the wall of fungi and blocks the oxidizing enzymes with the corresponding accumulation of peroxides and necrosis of the fungal cell. In vitro studies have shown a broad fungistatic and fungicidal activity. Like other azole agents, the spectrum of action of Fenticonazole also extends to some gram-positive bacteria such as Staphylococcus aureus. In vivo studies have also shown activity against Trichomonas Vaginalis.
Status:
Possibly Marketed Outside US
Source:
JAMA Netw Open. May 2024;7(5):e248661.: Phase 4 Human clinical trial Completed Vaginosis, Bacterial
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Dequalinium is a quaternary ammonium cation commonly available as the dichloride salt. Dequalinium chloride has an antiseptic effect against a wide range of bacteria, yeasts, and some fungi and viruses. It kills the micro-organisms associated with various mild infections of the mouth and throat. Also, Dequalinium chloride is active against the bacteria which cause bacterial vaginosis. Dequalinium Chloride (DECA) is a PKC inhibitor and high-affinity blocker CNGA1 channel, and nearly as effective on heteromeric CNGA1+CNGB1 channels. Common side effects are: vaginal discharge; vaginal itching or vaginal burning; vaginal yeast infection (thrush); tender tongue.
Status:
Possibly Marketed Outside US
Source:
CERVAGEM by Ono Pharmaceutical
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Gemeprost is a PGE1 analogue indicated for softening and dilatation of the cervix uteri prior to operative procedures or therapeutic abortion. The drug is marketed under the name Cervagem.
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:
NCT01822288: Phase 4 Interventional Completed Menopausal Syndromes
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tibolone (brand name Livial, Tibofem), also known as 7α-methylnoretynodrel, is a synthetic steroid drug with estrogenic, progestogenic, and weak androgenic actions which was introduced in 1988 and is used widely in Europe, Asia, Australasia, and, with the exception of the United States (where it is not available), the rest of the world. It is used mainly for treatment of endometriosis, as well as for the treatment of symptoms resulting from the natural or surgical menopause in post menopausal women. Women above 60 years of age should only start with LIVIAL treatment when they are intolerant of or contraindicated for other medicinal products approved for the treatment of oestrogen deficiency symptoms. Tibolone is used for the prevention of bone mineral density loss in postmenopausal women at high risk of future osteoporotic fractures who are intolerant of, or contraindicated for, other medicinal products approved for the prevention of bone mineral density loss. Tibolone has similar or greater efficacy compared to older hormone replacement drugs, but shares a similar side effect profile. It has also been investigated as a possible treatment for female sexual dysfunction. Tibolone is a 19-nortestosterone derivative and is related structurally to other 19-nortestosterone progestins. It is the 7α-methyl derivative of noretynodrel. Tibolone possesses a complex pharmacology. Its two major active metabolites, 3α-hydroxytibolone and 3β-hydroxytibolone, act as potent, fully activating agonists of the estrogen receptor (ER), with a high preference for ERα. Tibolone and its metabolite Δ-tibolone act as agonists of the progesterone and androgen receptors, while 3α-hydroxytibolone and 3β-hydroxytibolone, conversely, act as antagonists of these receptors. Lastly, tibolone, 3α-hydroxytibolone, and 3β-hydroxytibolone act as antagonists of the glucocorticoid and mineralocorticoid receptors, with preference for the mineralocorticoid receptor.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quingestanol is a metabolite of the quingestanol acetate, oral contraceptive, which was studied for therapy of menopausal diabetic women. Quingestanol is also a prodrug of norethisterone, which is used in birth control.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gestrinone is a synthetic trienic 19-norsteroid developed for the treatment of endometriosis. Gestrinone exerts its activity by activating androgen and progesterone receptors. The drug was approved for use in Latin America, Australia and Europe.
Status:
Possibly Marketed Outside US
Source:
NCT03745599: Phase 4 Interventional Completed Pain
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Benzydamine (benzydamine hydrochloride, PHARIXIA®) is a benzyl-indazole having analgesic, antipyretic, and anti-inflammatory effects. It is indicated for the relief of pain in acute sore throat and for the symptomatic relief of oro-pharyngeal mucositis caused by radiation therapy.
Status:
Possibly Marketed Outside US
Source:
Allynol by De Winter, M.S.|Siegmann, C.M.|Szpilfogel, S.A.
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Allylestrenol (INN) (brand names Gestanon, Gestanin, Orageston, Turinal, Gestin, others), or allyloestrenol (BAN), also known as 17α-allylestr-4-en-17β-ol or as 3-deketo-17α-allyl-19-nortestosterone, is a synthetic steroid with progestational activity, that is used to prevent threatened miscarriage, recurrent pregnancy loss, and premature labor. Allylestrenol has also been studied as a treatment for benign prostatic hyperplasia in men, with encouraging results. Although it is less potent as a progestogen relative to many other 19-nortestosterone derivatives, allylestrenol is said to be virtually devoid of androgenic, estrogenic, or glucocorticoid activity, and hence, unlike virtually all other 19-nortestosterone derivatives, appears to be a pure progestogen with similar effects to those of progesterone. Allylestrenol is widely marketed throughout Europe, including Russia and many other European countries, and is also available in Japan, Hong Kong, India, Bangladesh, Indonesia, and much of Southeast Asia, though notably not in the United States or Canada.
Status:
Possibly Marketed Outside US
Source:
NCT01065220: Phase 4 Interventional Completed Transsexualism
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Lynestrenol is a progestogen structurally related to norethisterone; it is used singularly, or as the progestogenic component of oral contraceptives. It is also used in treatments for menstrual disorders. Lynestrenol is typically used as an oral contraceptive, but also for the treatment of menstrual disorders like: Oligo-menorrhea and hypo-menorrhea; Polymenorrhoea; Fibrocystic mastopathy; Endometriosis; Endometrial carcinoma and/or metastases etc. As a synthetic oral progestogen, Lynestrenol has similar effects as that of the natural progesterone hormone. It has a strong progestational effect on the uterine endometrium by transforming the proliferative endometrium into a secretory one. It also inhibits the secretion of gonadotropin, suppresses maturation of follicles in the ovaries and ovulation, and reduces menstrual bleeding. Lynestrenol has minimal estrogenic, androgenic and anabolic effects.

Showing 141 - 150 of 194 results