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. 2021 Dec 24;14(1):87. doi: 10.3390/cancers14010087

Table 2.

Features of the multi kinase inhibitors approved by the Food and Drug Administration (FDA) from 2011 to 2021. The order of drugs is tabulated in order of most recent to the oldest registration date.

No. Generic Name of Drug Brand Name
and Company
First FDA/EMA Approved Date Structure Molecular Target Route of Administration Indication Adverse Effects Reference
1 Fedratinib INREBIC
Celgene Corporation, Summit, NJ, USA
FDA:
16 August 2019
EMA:
8 February 2021
graphic file with name cancers-14-00087-i005.jpg JAK2 2 Oral Myelofibrosis Diarrhea, nausea, vomiting, constipation, anemia, thrombocytopenia [66] 1, [67,68]
2 Gilteritinib XOSPATA
Astellas Pharma US, Inc., Northbrook, IL, USA
FDA:
28 November 2018
EMA:
24 October 2019
graphic file with name cancers-14-00087-i006.jpg FLT3 3,
AXL 4,
ALK 5
Oral Acute Myeloid Leukemia Myalgia, arthralgia, increased levels of transaminases, fatigue, malaise, fever, diarrhea, dyspnea, edema, rash, pneumonia, sepsis, renal impairment [69,70]
3 Midostaurin RYDAPT
Novartis Pharmaceuticals Corporation, East Hanover, NJ, USA
FDA:
28 April 2017
EMA:
18 September 2017
graphic file with name cancers-14-00087-i007.jpg c-Kit 6,
PDGFRA 7, PDGFRB 8, FLT3 3,
PKC 9, CDK1 10, SYK 11, VEGFR-2 12
Oral Acute Myeloid Leukemia, Cutaneous Mastocytosis Febrile neutropenia, nausea, vomiting, diarrhea, edema, mucositis, headache, device-related infection, abdominal pain, fatigue, pyrexia, dyspnea, musculoskeletal pain, constipation, epistaxis, upper respiratory tract infection, petechial, hyperglycemia, [71,72]
4 Ponatinib ICLUSIG
Ariad Pharmaceuticals, Inc., Cambridge, MA, USA
FDA:
14 December 2012
EMA:
1 July 2013
graphic file with name cancers-14-00087-i008.jpg BCR-ABL 13, VEGFRs 14, FGFRs 15, PDGFRs 16, RET 17,
c-Kit 6,
TIE2 18, FLT3 3
Oral Chronic Myelogenous
Leukemia, Acute
Lymphoblastic
Leukemia
Hypertension, cardiac failure, abdominal pain, constipation, diarrhea, oral mucositis, febrile neutropenia, fatigue, pneumonia, headache, peripheral neuropathy, dizziness, pleural effusion, cough, dyspnea, rush, dry skin, arthralgia, myalgia, spasms, decreased appetite, edema, weight loss, insomnia [73,74]
5 Ruxolitinib JAKAFI
Incyte Corporation, Wilmington, DE, USA
FDA:
16 November 2011
EMA:
23 August 2012
graphic file with name cancers-14-00087-i009.jpg JAK1 19, JAK2 2 Oral Myelofibrosis,
Polycythemia Vera,
Graft-versus-host disease
Anemia, thrombocytopenia, neutropenia [75,76]

1 Wrong chemical structure of the drug is given in the reference. 2 JAK2: Janus kinase 2. 3 FLT3: FMS-like tyrosine kinase-3. 4 AXL: AXL receptor tyrosine kinase. 5 ALK: anaplastic lymphoma kinase. 6 c-Kit: mast/stem cell growth factor receptor. 7 PDGFRA: platelet-derived growth factor receptor α. 8 PDGFRB: platelet-derived growth factor receptor β. 9 PKC: protein kinase C. 10 CDK1: cyclin-dependent kinase 1. 11 SYK: spleen tyrosine kinase. 12 VEGFR-2: vascular endothelial growth factor receptor-2. 13 BCR-ABL: BCR-ABL fusion protein. 14 VEGFRs: vascular endothelial growth factor receptors. 15 FGFRs: fibroblast growth factor receptors. 16 PDGFRs: platelet-derived growth factor receptors. 17 RET: receptor tyrosine kinase rearranged during transfection. 18 TIE2: tunica interna endothelial cell kinase 2. 19 JAK1: Janus kinase 1.