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

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Showing 3411 - 3420 of 4027 results

PHA-543613 was discovered by Pfizer and has been under development primarily as a potential treatment of schizophrenia. PHA-543613 acts as an agonist to the Neuronal acetylcholine receptor protein alpha-7 subunit. A single human trial was conducted in healthy human volunteers, but the compound has been studied extensively in rat models for schizophrenia as well as Parkinson's disease and Alzheimer's disease.
Status:
US Approved Allergenic Extract (1994)

Class (Stereo):
CHEMICAL (ACHIRAL)


Quaternium-15, a preservative, is one of the most used substances and is added to several cosmetics and other industrial products. Quaternium-15 is a mixture of isomers, where the cis-form is the dominant form and where the trans-form is the minor component present as an impurity. Quaternium-15 can be found under a variety of names, most commonly those of the Dow Chemical Company: Dowicil 200 (cis isomer only), Dowicil 75 and Dowicil 100 (both a mix of cis and trans isomers). The isolated cis-compound is used primarily in cosmetic applications, with a maximum permitted concentration in the EU of 0.2%. DOWICIL 200 preservative (cis form) is used primarily as a preservative in a wide variety of personal-care and cosmetic products. It is designed to provide highly effective broad-spectrum antimicrobial activity, especially in water-based formulations. It is used in both leave-on and rinse-off application such as baby-care products, hair-care products, lotions, powders, and creams. The mixed product (cis- and trans-) is used in a wider range of formulations such as: emulsifiable metal-cutting fluids; latex and emulsion paints; liquid floor polishes and floor waxes; glues and adhesives. Recently, the cis-form has been classified as a CMR substance with the classification toxic to reproduction, category 3. This classification only concerns the cis-isomer:
Clove oil is a natural product, derived from the Eugenia caryophyllata tree. Clove oil is 85 to 95% eugenol. Isoeugenol and methyleugenol make up 5 to 15% of the remaining ingredients. Isoeugenol is manufactured from eugenol by a process of isomerization. Isoeugenol have been used in foods and eugenol has been used in animal feeds. Isoeugenol is used as a fish anesthetic. The mechanism of action of isoeugenol in fish has not been determined. It is hypothesised that its effects are mediated via receptors controlling cellular ion channels in a similar way to that described for local anaesthetics. Reports of adverse reactions involving the use of isoeugenol in humans are primarily confined to incidents of contact sensitization or allergy following dermal exposure.
Status:
US Approved Allergenic Extract (1994)

Class (Stereo):
CHEMICAL (ACHIRAL)


Quaternium-15, a preservative, is one of the most used substances and is added to several cosmetics and other industrial products. Quaternium-15 is a mixture of isomers, where the cis-form is the dominant form and where the trans-form is the minor component present as an impurity. Quaternium-15 can be found under a variety of names, most commonly those of the Dow Chemical Company: Dowicil 200 (cis isomer only), Dowicil 75 and Dowicil 100 (both a mix of cis and trans isomers). The isolated cis-compound is used primarily in cosmetic applications, with a maximum permitted concentration in the EU of 0.2%. DOWICIL 200 preservative (cis form) is used primarily as a preservative in a wide variety of personal-care and cosmetic products. It is designed to provide highly effective broad-spectrum antimicrobial activity, especially in water-based formulations. It is used in both leave-on and rinse-off application such as baby-care products, hair-care products, lotions, powders, and creams. The mixed product (cis- and trans-) is used in a wider range of formulations such as: emulsifiable metal-cutting fluids; latex and emulsion paints; liquid floor polishes and floor waxes; glues and adhesives. Recently, the cis-form has been classified as a CMR substance with the classification toxic to reproduction, category 3. This classification only concerns the cis-isomer:
Propylparaben is a bacteriostatic and fungistatic agent used as a preservative in cosmetic products, food and drugs. As a food additive, it has the E number E216. To increase the activity and reduce its dose propylparaben is used in a mixture with other parabens and in combination with other types of preservatives. Propylparaben is a chemical allergen capable of producing immunologically mediated hypersensitivity reactions. Chemically it is an ester of p-hydroxybenzoic acid.
Status:
US Previously Marketed
First approved in 2023

Class (Stereo):
CHEMICAL (ACHIRAL)



Gepirone (brand name Travivo) is an investigational azapirone antidepressant and anxiolytic drug in development for the treatment of major depressive disorder but has yet to be marketed. Like other azapirones, it acts as a selective partial agonist of the 5-HT1A receptor. Gepirone has been under development in the U.S. in an extended release form (referred to as Gepirone ER). It has been rejected multiple times by the FDA during the drug approval process and Phase III studies evaluating its use in the treatment of MDD were prematurely terminated. These were the initial Phase III studies of gepirone ER in MDD, and the effective dose range had not been determined. In March 2016, the FDA reversed its decision and gave gepirone ER a positive review, clearing the way for the drug to finally gain market approval in the U.S. In addition to its antidepressant and anxiolytic properties, gepirone has been found to improve symptoms of sexual dysfunction in men and women, similarly to the marketed 5-HT1A receptor agonist flibanserin. The pro-sexual effects appear to be independent of its antidepressant and anxiolytic effects. Mechanism of action studies have demonstrated that gepirone possesses a much greater selectivity for 5-HT1A receptors over dopamine D2 receptors. Long-term studies have shown that gepirone has a differential action at presynaptic (agonist) and post-synaptic (partial agonist) 5-HT1A receptors. Treatment with gepirone ER desensitizes presynaptic 5-HT1A receptors, which decreases serotonin autoregulatory inhibition and enhances activation of postsynaptic 5-HT1A receptors. As a partial agonist gepirone ER acts as an agonist when endogenous serotonin is not present and as an antagonist when endogenous serotonin is present. Overall, gepirone ER increases serotonin production when insufficient amounts are present, and decreases serotonin production when excess amounts are present. Gepirone has been tested in Phase II clinical trial as antidepressant medication for pharmacotherapy for cocaine dependent subjects.
Status:
US Previously Marketed
First approved in 2022

Class (Stereo):
CHEMICAL (ACHIRAL)


Omidenepag isopropyl, a prodrug, is hydrolyzed in the eye to the active form (Omidenepag) which functions as a selective, nonprostaglandin, prostanoid EP2 agonist, has been developed by Ube Industries and Santen Pharmaceutical as an ophthalmic solution (EYBELIS®) for the treatment of glaucoma and ocular hypertension. Omidenepag isopropyl increases the outfow of aqueous humor via both the uveoscleral outfow and the trabecular outfow pathways, resulting in potent and stable reduction in intraocular pressure (IOP). In September 2018, omidenepag isopropyl ophthalmic solution 0.002% was approved in Japan for the treatment of glaucoma and ocular hypertension. On September 22, 2022, the FDA approved Santen’s Omlonti (omidenepag isopropyl), for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
Status:
US Previously Marketed
First approved in 2021

Class (Stereo):
CHEMICAL (ACHIRAL)



Mobocertinib (EXKIVITY™) is a first-in-class EGFR tyrosine kinase inhibitor being developed for the treatment of EGFR exon 20 insertion (EGFRex20ins) -positive non-small cell lung cancer (NSCLC). Mobocertinib is a kinase inhibitor of the epidermal growth factor receptor (EGFR) that irreversibly binds to and inhibits EGFR exon 20 insertion mutations at lower concentrations than wild type (WT) EGFR. Two pharmacologically-active metabolites (AP32960 and AP32914) with similar inhibitory profiles to mobocertinib have been identified in the plasma after oral administration of mobocertinib. In vitro, mobocertinib also inhibited the activity of other EGFR family members (HER2 and HER4) and one additional kinase (BLK) at clinically relevant concentrations (IC50 values <2 nM). Based on efficacy in patients whose disease had progressed on or after platinum-based therapy in a phase I/II trial, mobocertinib was recently granted accelerated approval in the USA in this indication. The drug is also being assessed for marketing approval in various other countries and territories including the EU and China.
Umbralisib (Ukoniq, TG Therapeutics) is an orally available PI3K delta inhibitor, targeting the delta isoform with nanomolar potency and several fold selectivity over the alpha, beta, and gamma isoforms of PI3K. The delta isoform of PI3K is strongly expressed in cells of hematopoietic origin and is believed to be important in the proliferation and survival of B-cell lymphocytes. On February 5, 2021, the Food and Drug Administration granted accelerated approval to umbralisib for the following indications: adult patients with relapsed or refractory marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen; adult patients with relapsed or refractory follicular lymphoma (FL) who have received at least three prior lines of systemic therapy. However, on June 1, 2022, the FDA withdrew its approval for the cancer medicine Ukoniq due to safety concerns.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(7) dandruff cresol, saponated
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


p-cresol, also known as also 4-methylphenol, is a unique bacterial metabolite from protein fermentation that is not produced by human enzymes, this metabolites has been frequently used to assess the degree of proteolytic fermentation. Recently investigation showed that p-cresol measurements might help to predict cardiovascular disease risk in renal patients over a wide range of residual renal function, beyond traditional markers of glomerular filtration. In addition, there were studies, which revealed, that urinary p-cresol was elevated in young French children with autism spectrum disorder.

Showing 3411 - 3420 of 4027 results