||Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model.
||A second-generation tyrosine kinase inhibitor of Bcr-Abl fusion protein and the platelet-derived growth factor receptor (PDGFR), with potential antineoplastic activity. Upon administration, radotinib specifically inhibits the Bcr-Abl fusion protein, an abnormal enzyme expressed in Philadelphia chromosome-positive chronic myeloid leukemia (CML) cells. In addition, this agent also inhibits PDGFR thereby blocking PDGFR-mediated signal transduction pathways. The inhibitory effect of radotinib on these specific tyrosine kinases may decrease cellular proliferation and inhibit angiogenesis. This agent has shown potent efficacy in CML cells that are resistant to the first-generation standard tyrosine kinase inhibitors, such as imatinib, nilotinib and dasatinib.
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DrugCentral Search Overview
Drug search example:
Generic drug names, drug synonyms, trade names terms can be used to search for drugs.
Example search for Lipitor can query using either “Atorvastatin” or “Lipitor”.A comprehensive list of drug development codes and salt or ester forms
are also stored in the database and can be used as search terms, for example search for "rosuvastatin" the following terms can be used: "rosuvastatin calcium" or "ZD4522".
Disease search example:
Supported disease terms are SNOMED-CT and OMOP vocabulary terms. Disease annotations for drugs approved before 2012 originate from OMOP vocabulary mappings. For drugs approved after 2012 disease annotations are extracted manually from approved drug labels and mapped to SNOMED-CT concepts.
Example search for “Chronic Hepatitis
returns the list of antiviral
indicated to treat “Chronic Hepatitis C” followed by drugs
contra-indicated in hepatitis C.
Target search example:
Supported target search terms are HUGO gene symbols, Uniprot accessions and target names, and Swissprot identifiers.
Example search for drugs targeting Mu-type opioid receptor can be run using either of the
terms: “OPRM1”, P35372, “OPRM
_HUMAN”, full or partial
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In collaboration with the IDG
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A - query term matched drug name or synonyms, mechanism of action target, or drug indication.
B - query term matched disease term in drug contraindications or off-label uses, targets listed in drug bioactivity profiles (not MoA targets), or pharmacologic action descriptions.
C - query term matched short drug description text.
D - query term matched full text in FDA drug labels.