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

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Showing 591 - 600 of 1216 results

Status:
US Previously Marketed
First approved in 1980

Class (Stereo):
CHEMICAL (RACEMIC)

Targets:


Oxamniquine is an anthelmintic with schistosomicidal activity against Schistosoma mansoni, but not against other Schistosoma spp. Oxamniquine is a potent single-dose agent for treatment of S. mansoni infection in man, and it causes worms to shift from the mesenteric veins to the liver, where the male worms are retained; the female worms return to the mesentery, but can no longer release eggs. Oxamniquine is a semisynthetic tetrahydroquinoline and possibly acts by DNA binding, resulting in contraction and paralysis of the worms and eventual detachment from terminal venules in the mesentry, and death. Its biochemical mechanisms are hypothesized to be related to an anticholinergic effect, which increases the parasite’s motility, as well as to synthesis inhibition of nucleic acids. Oxamniquine acts mainly on male worms, but also induces small changes on a small proportion of females. Like praziquantel, it promotes more severe damage of the dorsal tegument than of the ventral surface. The drug causes the male worms to shift from the mesenteric circulation to the liver, where the cellular host response causes its final elimination. The changes caused in the females are reversible and are due primarily to the discontinued male stimulation rather than the direct effect of oxamniquine
Status:
US Previously Marketed
First approved in 1974

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

Meglumine (N-methyl-D-glucamine) is a poorly metabolized derivative of sorbitol that has regulatory acceptance as a benign excipient for drug formulation to increase aqueous solubility of lipophilic drugs and improve their absorption. In conjugated form meglumine is used as a contrast agent.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(22)(ii) antifungal:diaper rash methylparaben
Source URL:
First approved in 1974

Class (Stereo):
CHEMICAL (ACHIRAL)



Methylparaben (E number E218) is preservative in the food, cosmetic, and pharmaceutical industries. It is completely absorbed through the skin or after ingestion and and it is hydrolyzed to para-hydroxybenzoic acid, and metabolites are rapidly excreted in the urine. Methylparaben is on the FDA generally regarded as safe list.
Status:
US Previously Marketed
Source:
21 CFR 310.532(a) benign prostatic hypertrophy alanine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Alanine is a non-essential aminoacid encoded by GCU, GCC, GCA, and GCG codons. Besides being a building block of proteins, alanine plays a key role in glucose-alanine cycle. Alanine is medically used as a dietary supplement for conditions such as fructose intolerance, muscle atrophy, low birth weight.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(20) weight control phenylalanine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Phenylalanine is a biologically essential amino acid that acts as a precursor to tyrosine and the catecholamines (epinephrine, norepinephrine, dopamine, and tyramine), and is a constituent of many central nervous system neuropeptides. Normal dietary levels of phenylalanine are approximately 1-2 grams daily. Phenylalanine appears in two forms which are identical mirror images of each other: L-phenylalanine, a nutritional supplement, and D-phenylalanine, an effective painkiller and antidepressant due to its ability to inhibit the breakdown of enkephalins, the brain’s natural pain killers.
Status:
US Previously Marketed
Source:
Alcopara by Burroughs Wellcome
(1967)
Source URL:
First approved in 1967
Source:
Alcopara by Burroughs Wellcome
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


BEPHENIUM HYDROXYNAPHTHOATE is an anthelmintic agent used in the treatment of hookworm and roundworm infections (Ancylostoma duodenale, Ascaris lumbricoides, and Necatore americanus). It targets the AChRs of nematodes producing spastic paralysis of the worms.
Thiabendazole (TBZ, trade names Mintezol, Tresaderm, and Arbotect) was first introduced in 1962. This drug is a fungicide and parasiticide and is indicated for the treatment of: strongyloidiasis (threadworm), cutaneous larva migrans (creeping eruption), visceral larva migrans, trichinosis: relief of symptoms and fever and a reduction of eosinophilia have followed the use of this drug during the invasion stage of the disease. But usage of this drug was discontinued. The precise mode of action of thiabendazole on the parasite is unknown, but it may inhibit the helminthspecific enzyme fumarate reductase. It was shown, also that thiabendazole reversibly disassembles newly established blood vessels, marking it as vascular disrupting agent (VDA) and thus as a potential complementary therapeutic for use in combination with current anti-angiogenic therapies. Was shown, that vascular disruption by TBZ results from reduced tubulin levels and hyper-active Rho signaling. In addition, was confirmed, that thiabendazole slowed tumor growth and decreased vascular density in preclinical fibrosarcoma xenografts and thus, it could lead directly to the identification of a potential new therapeutic application for an inexpensive drug that is already approved for clinical use in humans.
Status:
US Previously Marketed
Source:
SHADE UVAGUARD by BAYER HEALTHCARE LLC
(1992)
Source URL:
First approved in 1966
Source:
Solhar by Person-Covey
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Oxybenzone is one of the more popular molecules used by chemists during the manufacturing of cosmetics and is included in sunscreen for UV protection. The chemical is often used to stabilize and strengthen the color and scent of skin care products, but its widest use is in the form of sun block. Unfortunately, the debate about the safety of oxybenzone is still ongoing. One of the biggest concerns in the medical community about the widespread use of the molecule comes from the fact that it’s easily absorbed into the body. This absorption raises concerns that oxybenzone may accumulate in the body, eventually leading to potentially toxic levels of the chemical, which can affect the endocrine system.
Beta-carotene is found in many foods and is sold as a dietary supplement. Beta-carotene is a carotenoid, weak antioxidant; precursor of vitamin A, which is essential for vision and growth. Used to reduce the severity of photosensitivity reactions in patients with erythropoietic protoporphyria (EPP). Has been used in high-dose antioxidant supplements containing ascorbic acid and vitamin E with zinc in high-risk patients with age-related macular degeneration. Beta-carotene is also used to decrease asthma symptoms caused by exercise; to prevent certain cancers, heart disease, cataracts; and to treat AIDS, alcoholism, Alzheimer’s disease, depression, epilepsy, headache, heartburn, high blood pressure, infertility, Parkinson’s disease, rheumatoid arthritis, schizophrenia, and skin disorders including psoriasis and vitiligo.
Status:
US Previously Marketed
First approved in 1963

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Ropidoxuridine is a thymidine analogue and an oral prodrug of iododeoxyuridine that is easier to administer and less toxic with a more favorable therapeutic index in preclinical studies. Iododeoxyuridine demonstrated a survival advantage in Phase II studies in anaplastic astrocytoma, a type of brain tumor. Ropidoxuridine may help radiation therapy work better by making tumor cells more sensitive to the radiation therapy. In 2019, phase I clinical trials were ongoing to study the best dose of ropidoxuridine and its side effects in patients with metastatic malignant neoplasm in the brain and in patients with metastatic gastrointestinal cancer. First results showed that ropidoxuridine, combined with radiation therapy, was well-tolerated in patients with metastatic gastrointestinal cancer.