- 産業: Government; Health care
- Number of terms: 6957
- Number of blossaries: 0
- Company Profile:
The National Cancer Institute (NCI) is part of the National Institutes of Health (NIH), which is one of 11 agencies that compose the Department of Health and Human Services (HHS). The NCI, established under the National Cancer Institute Act of 1937, is the Federal Government's principal agency for ...
An orally available bromide salt form of butylscopolamine, a quaternary ammonium derivative of the alkaloid scopolamine, with anticholinergic property. Upon oral administration, hyoscine butylbromide binds to and blocks muscarinic receptors located on postganglionic parasympathetic nerve endings and on smooth muscle cells. This blocks the activity of acetylcholine (Ach) and causes its antispasmodic effect in the gastrointestinal (GI), urinary, uterine, and biliary tracts. This agent may also facilitate radiologic visualization of the GI tract.
Industry:Pharmaceutical
An orally available capsule-based nutritional supplement containing indole-3-carbinol, calcium-D-glucarate, Schizandra, vitamin D3, milk thistle, stinging nettle and hydroxymatairesinol (HMR) lignans, with potential estrogen modulating, antiproliferative and antioxidant activity. Indole-3-carbinol, found in vegetables of the Cruciferae family, may inhibit mammary cell growth and exerts antiestrogenic activity; Milk thistle (Silybum marianum) and Schizandra chinensis may enhance some of the phase II detoxification enzymes; calcium-D-glucarate and vitamin D3 may inhibit mammary cell growth; stinging nettle may exert its effect through its aromatase inhibiting activity; HMR lignans may have a beneficial effect on estrogen balance and levels. Therefore, ingredients in indole-3-carbinol/calcium/Schizandra/vitamin D3/milk thistle/stinging nettle/lignan-based nutritional capsule may alter estrogen balance and may protect against mammary carcinogenesis.
Industry:Pharmaceutical
An orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with potential antineoplastic activity. CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, thereby arresting the cell cycle in the G1 phase, suppressing DNA synthesis and inhibiting cancer cell growth. Overexpression of CDK4/6, as seen in certain types of cancer, causes cell cycle deregulation.
Industry:Pharmaceutical
An orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage. Syk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis.
Industry:Pharmaceutical
An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. INCB024360 targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.
Industry:Pharmaceutical
An orally available inhibitor of p70S6K signaling, with potential antineoplastic activity. P70S6K inhibitor LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation. P70S6K, a serine/threonine kinase, acts downstream of PIP3 and phosphoinositide-dependent kinase-1 in the PI3 kinase pathway, is often upregulated in a variety of cancer cells, and is involved in the regulation of cell growth, proliferation, motility, and survival.
Industry:Pharmaceutical
An orally available phosphodiesterase type 5 (PDE5) inhibitor with vasodilatory activity. Avanafil selectively inhibits PDE5, thus inhibiting the degradation of cyclic guanosine monophosphate (cGMP) found in the smooth muscle of the corpus cavernosa of the penis. The inhibition of cGMP degradation results in prolonged muscle relaxation, vasodilation, and blood engorgement of the corpus cavernosa, thereby prolonging penile erection.
Industry:Pharmaceutical
An orally available pyridopyrimidine-derived cyclin-dependent kinase (CDK) inhibitor with potential antineoplastic activity. PD-0332991 selectively inhibits cyclin-dependent kinases (particularly Cdk4/cyclin D1 kinase), which may inhibit retinoblastoma (Rb) protein phosphorylation; inhibition of Rb phosphorylation prevents Rb-positive tumor cells from entering the S phase of the cell cycle (arrest in the G1 phase), resulting in suppression of DNA replication and decreased tumor cell proliferation.
Industry:Pharmaceutical
An orally available selective antagonist of the endothelin-A (ET-A) receptor with potential antineoplastic activity. Zibotentan binds selectively to the ET-A receptor, thereby inhibiting endothelin-mediated mechanisms that promote tumor cell proliferation.
Industry:Pharmaceutical
An orally available small molecule dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs) with antiangiogenic and antineoplastic activities. VEGFR/PDGFR dual kinase inhibitor X-82 inhibits all isoforms of VEGFR and PDGFR, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and PDGFRs are receptor tyrosine kinases that may be upregulated in various tumor cell types. VEGFR/PDGFR dual kinase inhibitor X-82 has been shown to reduce tissue toxicity by 95 percent compared with first-generation kinase inhibitors.
Industry:Pharmaceutical
