Tyrosine kinases are a subclass of protein kinase. Tyrosine kinases play a central role in signal transduction that ultimately affects gene transcription within the nucleus. These molecules are considered as pivotal points of functional cellular pathways as they control cell cycle, proliferation, differentiation, and cell death or survival. Tyrosine kinases are primarily classified as receptor tyrosine kinase (RTK) which inlcude EGFR, PDGFR, FGFR and the IR and non-receptor tyrosine kinase (NRTK) which include SRC, ABL, FAK and Janus kinase. Disruption in tyrosine kinase pathway is implicated in several malignancies and thus tyrosine kinase inhibitors, targeted drug molecules inhibiting tyrosine kinase activity, are considered as a key therapeutic class. Few of the key marketed tyrosine kinase inhibitors include Dasatinib (Sprycel), Erlotinib (Tarceva), Gefitinib (Iressa), Imatinib (Gleevec). Lapatinib (Tykerb), Nilotinib (Tasigna), Sorafenib (Nexavar), Sunitinib (Sutent).
Over the past two decades, research studies have proved its efficacy for mitigation and control of non-cancerous diseases too. Thus research activity on use of inhibitors for various diseases such as Parkinson's disease and chronic obstructive pulmonary disorder is gradually increasing. The growing availability of these agents has enabled the pharmaceutical companies to develop new combination molecules which have the capacity to provide greater insight into the body’s acceptance of inhibitors so as to develop more effective therapies.
More recently, few molecules have been developed that inhibits tyrosine kinase these agents are in various stages of clinical development. The tyrosine kinase inhibitors pipeline has more than 15 molecules and is expected to achieve the regulatory approval in the near future, few of which are Oncoprex (CNVN202), ORS-1006, JNJ 49095397, RV-568, AP32788, APTO-500, and transtinib. In pipeline analysis, these are analyzed on the basis of route of administration (ROA) and type of molecule. The pipeline is also assessed based on monotherapy and combination therapy, and different clinical phases including Phase III, Phase II, Phase I and Pre-Clinical stage. Few of the companies which are involved in the development of tyrosine kinase inhibitor include IL-Yang Pharm, SRI, Sareum, Genprex, Arrien, J&J, and Takeda.
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