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

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Showing 81 - 90 of 1128 results

Estradiol an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Estradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estradiol is used for the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria). Estradiol is marketed under the brand name Climara (among others), indicated for: the treatment of moderate to severe vasomotor symptoms due to menopause, treatment of symptoms of vulvar and vaginal atrophy due to menopause, treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure and prevention of postmenopausal osteoporosis.
Status:
US Approved OTC
Source:
21 CFR 350.10(b) antiperspirant aluminum chlorohydrate
Source URL:
First marketed in 1921
Source:
Aluminum Hydroxide U.S.P.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Algeldrate (Aluminium hydroxide) is the amphoteric inorganic compound used as an antacid in the treatment of Duodenal, Peptic and Stomach Ulcer and some other conditions. Aluminium hydroxide is preferred over other alternatives such as sodium bicarbonate because Al(OH)3, being insoluble, does not increase the pH of stomach above 7 and hence, does not trigger secretion of excess acid by the stomach. Brand names include Alu-Cap, Aludrox, Gaviscon or Pepsamar. It reacts with the excess acid in the stomach, reducing the acidity of the stomach content, which may relieve the symptoms of ulcers, heartburn or dyspepsia. Such products can cause constipation, because the aluminum ions inhibit the contractions of smooth muscle cells in the gastrointestinal tract, slowing peristalsis and lengthening the time needed for stool to pass through the colon. Some such products (such as Maalox) are formulated to minimize such effects through the inclusion of equal concentrations of magnesium hydroxide or magnesium carbonate, which have counterbalancing laxative effects. This compound is also used to control phosphate (phosphorus) levels in the blood of people suffering from kidney failure. Precipitated aluminum hydroxide is included as an adjuvant in some vaccines (e.g. anthrax vaccine). One of the well-known brands of aluminum hydroxide adjuvant is Alhydrogel, made by Brenntag Biosector. Since it absorbs protein well, it also functions to stabilize vaccines by preventing the proteins in the vaccine from precipitating or sticking to the walls of the container during storage. Aluminium hydroxide is sometimes mistakenly called "alum", which properly refers to aluminum potassium sulfate. Vaccine formulations containing aluminum hydroxide stimulate the immune system by inducing the release of uric acid, an immunological danger signal. This strongly attracts certain types of monocytes which differentiate into dendritic cells. The dendritic cells pick up the antigen, carry it to lymph nodes, and stimulate T cells and B cells. It appears to contribute to induction of a good Th2 response, so is useful for immunizing against pathogens that are blocked by antibodies. In the 1960s and 1970s, it was speculated that aluminum was related to various neurological disorders including Alzheimer's disease. Since then, multiple epidemiological studies have found no connection between exposure to aluminum and neurological disorders.
Status:
US Approved OTC
Source:
21 CFR 358.110(b) wart remover:collodoin-like vehicle salicylic acid
Source URL:
First marketed in 1860
Source:
sodium salicylate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Methyl salicylate (or methyl 2-hydroxybenzoate), also known as wintergreen oil, is a natural product and is present in white wine, tea, porcini mushroom Boletus edulis, Bourbon vanilla, clary sage, red sage and fruits including cherry, apple, raspberry, papaya and plum. Methyl salicylate is topically used in combination with methanol and under brand name SALONPAS to temporarily relieves mild to moderate aches and pains of muscles and joints associated with: strains, sprains, simple backache, arthritis, bruises. The precise mechanism of action of methyl salicylate is not known, but there is suggested, that it cause dilation of the capillaries thereby increasing blood flow to the area.
Status:
Investigational
Source:
INN:zapnometinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03939689: Phase 2 Interventional Active, not recruiting Metastatic Prostate Cancer
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02783833: Phase 1/Phase 2 Interventional Completed Malaria
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Status:
Investigational
Source:
INN:naronapride [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naronapride (ATI-7505), an orally administered, cisapride analogue and serotonin4 (5HT4) receptor agonist, is being developed by Renexxion for the treatment of multiple gastrointestinal disorders. Sinovant is initially developing naronapride for the treatment of irritable bowel syndrome – constipation (IBS-C), a disease that affects millions of Chinese patients and for which few effective treatment options are available. Naronapride has been evaluated in over 900 subjects in multiple randomized controlled clinical studies and has demonstrated promising results in patients with gastroesophageal reflux disease (GERD), erosive esophagitis (EE), and chronic idiopathic constipation (CIC). Naronapride’s low systemic absorption and high specificity for 5HT4 and D2 receptors is thought to improve its safety and tolerability profile relative to other members of the class.
Status:
Investigational
Source:
INN:livoletide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Livoletide (AZP-531) is an analog of unacylated ghrelin, a naturally occurring hormone that is thought to counteract the effects of acylated ghrelin. The drug was designed to improve glycaemic control and reduce weight. Livoletide participated in pivotal phase 2b/3 clinical study for the treatment of Prader-Willi syndrome. In addition, the drug was studied in patients with type 2 diabetes mellitus (T2D). Its pharmacokinetic profile, suitable for once daily dosing, and metabolic effects support further clinical development for T2D.
Status:
Investigational
Source:
INN:implitapide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Implitapide is a microsomal triglyceride transfer protein (MTP) inhibitor with antihyperlipidemic activity. Microsomal triglyceride transfer protein (MTP) is essential for the synthesis of both chylomicron in the intestine and very low-density lipoprotein in the liver. In an animal model, inhibition of MTP by implitapide reduced both total cholesterol and triglyceride levels and suppressed progression of atherosclerotic lesions in apolipoprotein E knockout mice fed a Western-type diet.