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

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Showing 141 - 150 of 276 results

Status:
Other

Class (Stereo):
CHEMICAL (ABSOLUTE)

Estramustine is an antineoplastic agent indicated in the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate. Estramustine is a combination of estradiol with nitrogen mustard. In vivo, the nitrogen-mustard moiety becomes active and participates in alkylation of DNA or other cellular components. This causes DNA damage in rapidly dividing cancerous cells leading to cell death and ideally, tumor shrinkage. Also, due to the drugs estrogen component, it can bind more selectively to active estrogen receptors. Used for the palliative treatment of patients with metastatic and/or progressive carcinoma of the prostate.
Status:
US Previously Marketed
Source:
Thiouracil by Lilly
(1946)
Source URL:
First approved in 1946
Source:
Thiouracil by Lilly
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Thiouracil or 2-thiouracil was introduced in 1943 as the first thionamide anti-thyroid drug. Owing to a high frequency of adverse reactions, especially agranulocytosis, use of thiouracil was abandoned in favor of other, less toxic drugs. Thiouracil is not currently used as a thyrostatic drug in humans. Thiouracil inhibits thyroid activity by blocking the enzyme thyroid peroxidase. It is also it is a highly selective inhibitor of neuronal nitric oxide synthase, by interfering with the substrate- and tetrahydrobiopterin (BH(4))-binding to the enzyme. Due to its ability selectively accumulating in de novo-synthesized melanin in overactive melanin-producing cells and thus providing a means to localize melanoma cells, thiouracil can represent a useful new tool to identify modulators of human hair pigmentation.
Status:
US Previously Marketed
Source:
21 CFR 310.545(a)(6)(ii)(A) cough/cold:nasal decongestant allyl isothiocyanate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Allyl isothiocyanate (AITC), also known as mustard oil, is one of the most common naturally occurring isothiocyanates, which occurs in many common cruciferous vegetables. Besides antimicrobial activity against a wide spectrum of pathogens, it showed anticancer activity in both cultured cancer cells and animal models, although the underlining mechanisms remain largely undefined. Allyl isothiocyanate is a TRPA1 and TRPV1 agonist and pungency and lachrymatory effects of Allyl isothiocyanate are mediated through the TRPA1 and TRPV1 ion channels. Allyl isothiocyanate irritates the mucous membranes and induces eczematous or vesicular skin reactions.
Orotic acid is a minor dietary constituent. Historically it was believed to be part of the vitamin B complex and was called vitamin B13, but it is now known that it is not a vitamin and is synthesized in the body, where it arises as an intermediate in the pathway for the synthesis of pyrimidine nucleotides. Orotic acid is converted to UMP by UMP synthase, a multifunctional protein with both orotate phosphoribosyl transferase and orotidylate decarboxylase activity. The most frequently observed inborn error of pyrimidine nucleotide synthesis is a mutation of the multifunctional protein UMP synthase. As a result, plasma orotic acid accumulates to high concentrations, and increased quantities appear in the urine. Orotic acid levels are elevated in the urea cycle defects ornithine transcarbamylase (OTC) deficiency, citrullinemia and argininosuccinic acidemia, as well as the mitochondrial transport disorder hyperornithinemia-hyperammonemia-homocitrullinuria (HHH) syndrome. Orotic acid is also elevated in hereditary orotic aciduria, or uridine monophosphate synthase deficiency, an autosomal recessive disorder characterized by megaloblastic anemia and crystalluria. In addition, orotic acid in combination with leflunomide is in the phase II of clinical trial to evaluate the clinical efficacy and safety of a combination in kidney transplant patients with high levels of Polyoma BK viruria for the purpose of preventing polyoma BK viremia and nephropathy, that could lead to kidney transplant loss from viral damage, acute rejection or both.
Status:
Possibly Marketed Outside US
Source:
Cellapy Haircell Meso Tonic by Gm Holdings Co., Ltd
(2016)
Source URL:
First approved in 2010

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Possibly Marketed Outside US
Source:
AGELOC TRANSFORMATION by Liebig, J.
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Creatinine is a product of metabolism of creatine phosphate, a molecule that serves as a rapidly mobilizable reserve of a brain and skeletal muscle. Creatinine is excreted by kidneys with little or no reabsorption. Serum creatinine is the most commonly used indicator of renal function.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ABSOLUTE)

Atrimustine [bestrabucil, busramustine, KM 2210, kregan], a conjugate of estradiol and chlorambucil, is a DNA antagonist that was developed by Kureha Corporation (Japan). Atrimustine is an antineoplastic drug that was used for the treatment of breast cancer, non-Hodgkin's lymphoma, as well as Graft-versus-host disease. Side effects of atrimustine in clinical trials included vaginal bleeding and gynecomastia. Atrimustine reached preregistration in Japan for the treatment of cancer, however, its development has been discontinued.
Status:
Possibly Marketed Outside US
Source:
NCT02887365: Phase 4 Interventional Unknown status MSI-L/MSS
(2014)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (RACEMIC)

Trofosfamide is an orally bioavailable antineoplastic agent. Upon administration, it is predominantly metabolized to the cyclophosphamide analog ifosfamide, which is then metabolized by liver cytochrome P450s to the active isophosphoramide mustard (IPM). IPM alkylates DNA to form DNA-DNA cross-links, which may result in inhibition of DNA, RNA and protein synthesis, and tumor cell apoptosis. Trofosfamide is marketed in Germany by Baxter under tradename Ixoten. It is indicated for the treatment of non-Hodgkin's lymphoma after failure of the standard therapy. The drug was investigated in the clinical trials against soft tissue sarcoma and melanoma.

Showing 141 - 150 of 276 results