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

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Showing 371 - 380 of 1076 results

Angelicin (isopsoralen), is a furocoumarin, occuring in a number of plants belonging to the Umbelliferae family. It acts as a photosensitizer by forming DNA monoadducts. Angelicin is able to inhibit monoamine oxidase (MAO) activities in rat brain mitochondria. Angelicin exerts antineoplastic and antidiabetic properties in animal models.
Status:
Possibly Marketed Outside US
Source:
Anti aging by XIAN CHIANG COMPANY LIMITED
(2023)
Source URL:
First approved in 2023
Source:
Anti aging by XIAN CHIANG COMPANY LIMITED
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Fisetin, a natural flavonoid found in various fruits, vegetables, and nuts, has various biological properties, including anti-inflammatory, anti-oxidant, neuroprotective in cell culture and in animal models relevant to human diseases. Fisetin can be also a promising agent for the treatment of uveal melanoma. Besides, it is a therapeutic agent for respiratory inflammatory diseases such as chronic obstructive pulmonary disease (COPD), where fisetin inhibits the TNF-α-activated IKK/NF-κB cascade by targeting PKCδ. In vitro and in vivo experiments have revealed that fisetin possesses significant therapeutic effects against diabetic complications and atherosclerosis, where it can suppress vascular inflammatory processes.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Flotufolastat F 18 (POSLUMA®) is an 18F-labelled radiohybrid (rh) prostate-specific membrane antigen (PSMA)-targeted imaging agent being developed by Blue Earth Diagnostics, a subsidiary of Bracco Imaging, for prostate cancer imaging. In May 2023, flotufolastat F 18 received its first approval in the USA as a radioactive diagnostic agent for positron emission tomography (PET) of PSMA positive lesions in men with prostate cancer with suspected metastasis who are candidates for initial definitive therapy or with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level. Flotufolastat F 18 binds to PSMA (IC50 = 4.4 nM) expressed on cells, including prostate cancer cells, and is internalized. Prostate cancer cells usually overexpress PSMA. Fluorine-18 is a beta emitting radionuclide that can be detected using positron emission tomography.
Status:
Possibly Marketed Outside US
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
(2021)
Source URL:
First approved in 2021
Source:
Hepad S5 by YOUNGJIN Korean Medicine Clinic
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Proximadiol was isolated from the rhizomes of Zingiber mekongense and leaves of Blumea balsamifera. Compound lacks ativiral and antibacterial activity. Proximadiol was found to inhibit platelet-activating factor receptor binding on platelets at micromolar concentrations.
Status:
Possibly Marketed Outside US
First approved in 2020

Class (Stereo):
CHEMICAL (ACHIRAL)


Diflubenzuron is a direct-acting insecticide normally applied directly to plants or water. Diflubenzuron, besides its use in agriculture, horticulture and forestry against larvae of Lepidoptera, Coleoptera, Diptera, Hymenoptera, and in public health against larvae of mosquitoes, is used as a veterinary drug for the treatment of sea lice infestations in Atlantic salmon. Diflubenzuron acts by interference with the synthesis of chitin. It is reported that public exposure to diflubenzuron through either food or drinking-water is negligible.
Status:
Possibly Marketed Outside US
Source:
NCT03238105: Phase 4 Interventional Unknown status Periorbital Disorder
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Thioglycolic acid (TGA, also known as MERCAPTOACETIC ACID) is widely used in the hairdressing industry, which mostly caters to women. TGA has been reported to impair several organs, especially reproductive ones such as testes and ovaries. Thioglycolates (the salt forms of TGA) was shown to penetrate the skin and distribute to the kidneys, lungs, small intestine, and spleen; excretion is primarily in the urine. In addition, thioglycolates can be skin irritants of an animal and can be sensitizers.
Retinal, All-trans is one of the forms of vitamin A. It is an isomer of 11-cis-retinal, transductor of light into the neural signals. Retinal, All-trans is converted to retinoic acid in vivo by the action of retinal dehydrogenase. Retinal, All-trans is associated with one of the two isoforms of cellular retinol-binding proteins (CRBP-I and CRBP-II). These proteins play important roles in retinoid biology and regulation of the metabolism of retinol and retinal.
Status:
Possibly Marketed Outside US
Source:
NCT01056042: Phase 4 Interventional Completed Endometriosis
(2007)
Source URL:
First approved in 2018

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Gestodene (17alpa-ethynyl-13beta-ethyl-17beta-hydroxy-4,15-gonadien-3-one) is the most potent synthetic progestin currently available and it is widely used as a fertility regulating agent in a number of contraceptive formulations because of its high effectiveness, safety and acceptability. Products containing gestoden include Meliane, which contains 20 ug of ethinylestradiol and 75 ug of gestodene; and Gynera, which contains 30 ug of ethinylestradiol and 75 ug of gestodene. Gestodene is androgenically neutral, meaning that contraceptive pills containing gestodene do not exhibit the androgenic side effects (e.g. acne, hirsutism, weight gain) often associated with second-generation contraceptive pills. Gestodene displays a high binding affinity to the progesterone receptor, also binds to adrogen and glucocorticoid receptors but no measurable affinity for the estrogen receptor.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)



Shikimic acid (SA), an active metabolite of polyphenol-rich food intake, originally extracted from Illicium verum Hook. fil. is an indispensable starting material for the synthesis of the antiviral drug oseltamivir and others useful compounds. In the biological studies, SA has been reported to have anti-inflammatory, analgesia, antioxidant, antithrombotic, and antibacterial activities. SA can play an important role in reducing platelet activation, aggregation related thrombus formation and biomarkers of thrombogenesis in sedentary individuals. In addition, was investigated antibacterial activity of SA against S. aureus, which could be caused by the interactions of SA with S. aureus membrane proteins and lipids, resulting in causing cell membrane dysfunction and bacterial damage or even death.
Status:
Possibly Marketed Outside US
First approved in 2018

Class (Stereo):
CHEMICAL (ACHIRAL)



Flubendazole is an anthelmintic that is used to treat worm infection in humans. It is available OTC in Europe. Flubendazole is registered and sold in Europe (EMEA) as Fluvermal (Johnson and Johnson, Sante Bea). A 100mg dose of Fluvermal is most commonly proscribed for treating pinwoms (Enterobius vermiculus)). This is followed by a second dose of 100mg 15-21 days later to ensure reinfection is avoided, as flubendazole does not kill pinworm eggs. 100mg taken 3 times a day for 3 days is effective against larger nematodes, but only marginally effective against tapeworms. Flubendazole was validated for its anti-proliferative efficacy in MDA-MB-231 cells. Moreover, Flubendazole induced autophagy and increased ROS production. In silico analysis and experimental validation together demonstrate that Flubendazole can target autophagy-related protein 4B (Atg4B) in MDA-MB-231 cells and induce autophagy, which may shed light on the exploration of this compound as a potential new Atg4B targeted drug for future triple-negative breast cancer (TNBC) therapy.