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

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 1 - 10 of 17 results

Selumetinib (AZD6244 or ARRY-142886) is a potent, selective, and ATP-uncompetitive inhibitor of Ras-Raf-mitogen-activated protein kinase kinase (MEK1/2). This inhibition can prevent ERK activation, disrupt downstream signal transduction, and inhibit cancer cell proliferation and survival. Selumetinib has shown tumour suppressive activity in multiple rodent models of human cancer including melanoma, pancreatic, colon, lung, and breast cancers. AstraZeneca is responsible for development and commercialization of selumetinib.
Vandetanib, 4-anilinoquinazoline, is an anti-cancer drug that with the potential for use in a broad range of tumour types. In 2011 vandetanib (trade name Caprelsa) was approved by the FDA to treat nonresectable, locally advanced, or metastatic medullary thyroid cancer in adult patients. In vitro studies have shown that vandetanib inhibits the tyrosine kinase activity of the EGFR and VEGFR families, RET, BRK, TIE2, and members of the EPH receptor and Src kinase families. These receptor tyrosine kinases are involved in both normal cellular function and pathologic processes such as oncogenesis, metastasis, tumor angiogenesis, and maintenance of the tumor microenvironment. Vandetanib was shown to inhibit epidermal growth factor (EGF)-stimulated receptor tyrosine kinase phosphorylation in tumor cells and endothelial cells and VEGF-stimulated tyrosine kinase phosphorylation in endothelial cells. Vandetanib administration reduced tumor cell-induced angiogenesis, tumor vessel permeability, and inhibited tumor growth and metastasis in mouse models of cancer.
CUDC-907 is a small molecule inhibitor of histone deacetylase and PI3 kinase developed by Curis. It is investigated in clinical trials for the treatment of relapsed or refractory lymphomas, thyroid cancer, multiple myeloma, breast cancer and other malignancies.
Motesanib (AMG 706), a novel nicotinamide, was identified as a potent, orally bioavailable inhibitor of the VEGFR1/Flt1, VEGFR2/kinase domain receptor/Flk-1, VEGFR3/Flt4 and Kit receptors. Motesanib was expected to reduce vascular permeability and blood flow in human tumours. A phase III trial of motesanib in combination with paclitaxel and carboplatin in non-squamous NSCLC has been terminated by Takeda and subsequently the development was discontinued. Motesanib has also been investigated up to phase II in breast, thyroid, colorectal and gastrointestinal stromal tumours. However, development has been discontinued in these indications.
Status:
Investigational
Source:
INN:broquinaldol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Broquinaldol is a halogenated derivative of quinoline and a member of the class of compounds known as halogenated phenazines. Broquinaldol and related compounds have demonstrated efficacy against antibiotic-tolerant bacterial biofilms and Mycobacterium tuberculosis. Against several bacterial strains, broquinaldol had a minimum inhibitory concentration of 0.78 microM. Broquinaldol was also identified as having antiproliferative activity against thyroid cancer cells in vitro.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

PLX-4720 is a pre-clinical analog of vemurafenib which selectively targets BRAFV600E. PLX-4720 was developed by Plexxikon for the treatment of thyroid cancer, however the drug did not reach clinical phase.
First synthesized in 2004 by the group of Peter G. Schultz, reversine is a 2,6- diamino substituted purine showing a potent inhibition on Aurora B, a protein kinase overexpressed in a variety of solid tumors. Due to its relevance in the cell cycle regulation, Aurora B represents a good target for anti-cancer drug development, so that reversine can be used as a promising lead compound for new potential antitumor agents. Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Reversine also inhibits Mps1. Reversine is effective in inhibiting the growth of thyroid cancer cells by cell cycle arrest or apoptosis, especially with the more aggressive ATC and PDTC. Apoptosis was induced by the mitochondria-independent pathway. Reversine is being under investigation in clinical therapeutics.
6-Methoxy-2-naphthalenecarboxaldehyde is a substrate of aldehyde dehydrogenase enzymes (class I, class II and class III). It was examined as indicator of the aldehyde dehydrogenase (ALDH) activity in human tissue homogenates and accessible body fluids from patients with viral and toxic liver injuries, and tumors. As intermediate, it was used in organic synthesis of enantiomerically enriched R- and S-6-MONCH- (OH)CN and fluorescent substrates for inhibition studies relating to hypertension and vascular inflammation.
Status:
Possibly Marketed Outside US
Source:
SODIUM IODIDE I 123 by Svoboda, K.
Source URL:
First approved in 2012

Class (Stereo):
CHEMICAL (ACHIRAL)


IODINE I-123 is a radioactive isotope of iodine used in nuclear medicine imaging, including single photon emission computed tomography (SPECT) and X-ray computed tomography (X-Ray CT) scans. Iodine-123 is usually supplied as sodium iodide (NaI) and hypoiodite (OI−) in dilute sodium hydroxide solution, at high isotopic purity. 123I is the most suitable isotope of iodine for the diagnostic study of thyroid diseases. The half-life of approximately 13.13 h (hours) is ideal for the 24-h (hour) iodine uptake test and 123I has other advantages for diagnostic imaging thyroid tissue and thyroid cancer metastasis. The iodine is taken up by the thyroid gland and/or cancer metastasis and a gamma camera is used to functional images of the thyroid for diagnosis. Quantitative measurements of the thyroid can be performed to calculate the iodine uptake (absorption) for the diagnosis of hyperthyroidism and hypothyroidism. This is administered to a patient in capsule form, by intravenous injection, or in a drink.
Status:
Possibly Marketed Outside US
Source:
Japan:Aclarubicin Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Aclarubicin (INN) or aclacinomycin A is an anthracycline drug is primarily indicated in conditions like Acute non-lymphoblastic leukemia, Breast cancer, Gastric cancer, Lymphoma, Ovarian coma, Small cell lung cancer, Thyroid cancer. Soil bacteria Streptomyces galilaeus can produce aclarubicin. Aclarubicin (HCl) is used in combination with different anticancerous drugs to obtain best therapeutic results and to reduce toxicity or side effects. Aclarubicin (HCl) is administered intravenously. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.

Showing 1 - 10 of 17 results