Tyrosine Kinase Inhibitor
43 Topics FoundNeratinib (INN), sold under the brand name Nerlynx, is a tyrosine kinase inhibitor anti-cancer medication used for the treatment of breast cancer.[2][3] The most common side effect is diarrhea, which affects nearly all patients.[3] Other common side effects include nausea (feeling sick), vomiting, tiredness, belly pain, rash, decreased appetite, stomatitis (sore, inflamed mouth), and muscle spasms.[3] Contents 1 Medical uses 2 ...
Axitinib, sold under the brand name Inlyta, is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models[3] and has shown partial responses in clinical trials with renal cell carcinoma (RCC)[4] and several other tumour types.[5] It was approved to treat renal cell carcinoma by the U.S. Food and Drug Administration after showing a modest increase...
Axitinib, sold under the brand name Inlyta, is a small molecule tyrosine kinase inhibitor developed by Pfizer. It has been shown to significantly inhibit growth of breast cancer in animal (xenograft) models[3] and has shown partial responses in clinical trials with renal cell carcinoma (RCC)[4] and several other tumour types.[5] It was approved to treat renal cell carcinoma by the U.S. Food and Drug Administration after showing a modest increase...
Neratinib (INN), sold under the brand name Nerlynx, is a tyrosine kinase inhibitor anti-cancer medication used for the treatment of breast cancer.[2][3] The most common side effect is diarrhea, which affects nearly all patients.[3] Other common side effects include nausea (feeling sick), vomiting, tiredness, belly pain, rash, decreased appetite, stomatitis (sore, inflamed mouth), and muscle spasms.[3] Contents 1 Medical uses 2 ...
Fostamatinib, sold under the brand names Tavalisse and Tavlesse, is a tyrosine kinase inhibitor medication for the treatment of chronic immune thrombocytopenia (ITP).[1][2] The drug is administered by mouth.[1][2] Fostamatinib blocks the activity of the enzyme spleen tyrosine kinase (SYK).[2] This enzyme is involved in stimulating parts of the immune system.[2] By blocking SYK's activity, fostamati...
Fostamatinib, sold under the brand names Tavalisse and Tavlesse, is a tyrosine kinase inhibitor medication for the treatment of chronic immune thrombocytopenia (ITP).[1][2] The drug is administered by mouth.[1][2] Fostamatinib blocks the activity of the enzyme spleen tyrosine kinase (SYK).[2] This enzyme is involved in stimulating parts of the immune system.[2] By blocking SYK's activity, fostamati...
Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Since 2009 it was studied as a potential treatment option in multiple tumor types.[1] By 2015 it had two US approvals for advanced cancers. Contents 1 Approvals and indications...
Regorafenib, sold under the brand name Stivarga among others, is an oral multi-kinase inhibitor developed by Bayer which targets angiogenic, stromal and oncogenic receptor tyrosine kinase (RTK). Regorafenib shows anti-angiogenic activity due to its dual targeted VEGFR2-TIE2 tyrosine kinase inhibition. Since 2009 it was studied as a potential treatment option in multiple tumor types.[1] By 2015 it had two US approvals for advanced cancers. Contents 1 Approvals and indications...
Bosutinib (rINN/USAN; codenamed SKI-606, marketed under the trade name Bosulif) is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia. Originally synthesized by Wyeth, it is being developed by Pfizer. Contents 1 Mechanism 2 Medical uses 3 Contraindications 4 Interactions 5 Notes 6 See also 7 References 8 External links Mechanism It is an ATP-competitive Bcr-Abl tyrosine-kinase inhibitor with an additional inhibitory effect...
Bosutinib (rINN/USAN; codenamed SKI-606, marketed under the trade name Bosulif) is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia. Originally synthesized by Wyeth, it is being developed by Pfizer. Contents 1 Mechanism 2 Medical uses 3 Contraindications 4 Interactions 5 Notes 6 See also 7 References 8 External links Mechanism It is an ATP-competitive Bcr-Abl tyrosine-kinase inhibitor with an additional inhibitory effect...
Gilteritinib, sold under the brand name Xospata, is an anti-cancer drug.[6] It acts as an inhibitor of FLT3, hence it is a tyrosine kinase inhibitor.[7] It was developed by Astellas Pharma. In April 2018, Astellas filed a new drug application with the Food and Drug Administration for gilteritinib for the treatment of adult patients with FLT3 mutation–positive relapsed or refractory acute myeloid leukemia (AML).[8] In November 2018, the ...
Gilteritinib, sold under the brand name Xospata, is an anti-cancer drug.[6] It acts as an inhibitor of FLT3, hence it is a tyrosine kinase inhibitor.[7] It was developed by Astellas Pharma. In April 2018, Astellas filed a new drug application with the Food and Drug Administration for gilteritinib for the treatment of adult patients with FLT3 mutation–positive relapsed or refractory acute myeloid leukemia (AML).[8] In November 2018, the ...
Sunitinib, sold under the brand name Sutent, is a medication used to treat cancer.[1] It is a small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications.[2] As of August 2021, sunitinib is available as a...
Sunitinib, sold under the brand name Sutent, is a medication used to treat cancer.[1] It is a small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST) on January 26, 2006. Sunitinib was the first cancer drug simultaneously approved for two different indications.[2] As of August 2021, sunitinib is available as a...
Pazopanib, sold under the brand name Votrient, is an anti-cancer medication marketed worldwide by Novartis. It is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by numerous regulatory administrations worldwide.[3][4][5][6] Contents 1 Medical uses 2 Contraindications 3 Adverse effec...
Erdafitinib, sold under the brand name Balversa, is an anti-cancer medication. It is a small molecule inhibitor of fibroblast growth factor receptor (FGFR) used for the treatment of cancer. FGFRs are a subset of tyrosine kinases which are unregulated in some tumors and influence tumor cell differentiation, proliferation, angiogenesis, and cell survival.[1][2] Astex Pharmaceuticals discovered the drug and licensed it to Janssen Pharmaceuticals for further develo...
Erdafitinib, sold under the brand name Balversa, is an anti-cancer medication. It is a small molecule inhibitor of fibroblast growth factor receptor (FGFR) used for the treatment of cancer. FGFRs are a subset of tyrosine kinases which are unregulated in some tumors and influence tumor cell differentiation, proliferation, angiogenesis, and cell survival.[1][2] Astex Pharmaceuticals discovered the drug and licensed it to Janssen Pharmaceuticals for further develo...
Pazopanib, sold under the brand name Votrient, is an anti-cancer medication marketed worldwide by Novartis. It is a potent and selective multi-targeted receptor tyrosine kinase inhibitor that blocks tumour growth and inhibits angiogenesis. It has been approved for renal cell carcinoma and soft tissue sarcoma by numerous regulatory administrations worldwide.[3][4][5][6] Contents 1 Medical uses 2 Contraindications 3 Adverse effec...
Pacritinib, sold under the brand name Vonjo, is an anti-cancer medication used to treat myelofibrosis.[1][2] It is a macrocyclic Janus kinase inhibitor. It mainly inhibits Janus kinase 2 (JAK2) and Fms-like tyrosine kinase 3 (FLT3). Common side effects include diarrhea, low platelet counts, nausea, anemia, and swelling in legs.[2] Contents 1 Medical uses 2 History 3 Society and culture 3.1 Names 4 References 5 External links Medical us...
Pralsetinib, sold under the brand name Gavreto, is a medication for the treatment of metastatic RET fusion-positive non-small cell lung cancer (NSCLC).[3] Pralsetinib is a tyrosine kinase inhibitor. It is taken by mouth.[3] The most common adverse reactions include increased aspartate aminotransferase (AST), decreased hemoglobin, decreased lymphocytes, decreased neutrophils, increased alanine aminotransferase (ALT), increased creatinine, increased alkaline phos...