Inhibitor Drugs
Many inhibitor drugs used to treat cancer are kinase inhibitors based on the tyrosine substrate. They are called tyrosine kinase inhibitors or tyrphostins (short name for “tyrosine phosphorylation inhibitor).
Afatinib
Brand/Trade Names: Gilotrif
Formula: C24H25ClFN5O3
Manufacturers: Alembic Pharmaceuticals Limited, Biotechnica Pharma Global, Epoch Labs, Fresenius Kabi Oncology Limited
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: EGFR inhibitor. Approved by the FDA in 2013. Approved for treatment of non-small cell lung cancer.
Asciminib
Brand/Trade Names: Scemblix
Formula: C20H8ClF2N5O3
Manufacturers: Novartis
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class:
Administration: Oral
Notes:Approved by the FDA in 2021. Approved for treatment of leukemia.
Avapritinib
Brand/Trade Names: Ayvakit
Formula: C26H27FN10
Manufacturer: Blueprint Medicines Corporation
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2020. Approved for treatment of stomach cancer.
Axitinib
Brand/Trade Names: Inlyta
Formula: C22H18N4OS
Manufacturers: U.S. Pharmaceuticals, Alembic Pharmaceuticals Limited, Biotechnica Pharma Global, Cipla
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: Approved by the FDA in 2012. VEGF inhibitor and angiogenesis inhibitor. Used for treatment of renal cell carcinoma.
Cabozantinib
Brand/Trade Names: Cometriq
Formula: C28H24FN3O5
Manufacturers: Exelixis, Fermion Oy, Guangzhou Tosun Pharmaceutical, Hetero Drugs Limited
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2012. Angiogenesis inhibitor. Used for treatment of renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer.
Capmatinib
Brand/Trade Names: Tabrecta
Formula: C23H17FN6O
Manufacturer: Novartis Oncology
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2020. Used for non smell-cell lung cancer.
Dacomitinib
Brand/Trade Names: Vizimpro
Formula: C24H25ClFN5O2
Manufacturers: U.S. Pharmaceuticals, MSN Laboratories Pvt Ltd, Pfizer Laboratories Div Pfizer Inc
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: Approved by the FDA in 2018. EGFR inhibitor and HER inhibitor. Used for treatment of non-small cell lung cancer.
Entrectinib
Brand/Trade Names: Rozlytrek
Formula: C31H34F2N6O2
Manufacturers: Johnson Matthey PLC, Sun-shine Chem, Genentech Inc.
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: Approved by the FDA in 2019. Tumor-agnostic drug.
Infigratinib
Brand/Trade Names: Truseltiq
Formula: C26H31Cl2N7O3
Manufacturers: QED Therapeutics
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I½
Administration: Oral
Notes: Approved by the FDA in 2021 for cancer of the bile duct.
Mobocertinib
Brand/Trade Names: Exkivity
Formula: C32H39N7O4
Manufacturers: Takeda
Mechanism: Kinase Inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: Approved by the FDA in 2021 for lung cancer.
Osimertinib
Brand/Trade Names: Tagrisso
Formula: C28H33N7O2
Manufacturers: AstraZeneca Pharmaceuticals LP, Epoch Labs, Mylan Inc, Shanghai Hope Chem
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: EGFR inhibitor. Approved by the FDA in 2015. Used for treatment of non-small cell lung cancer.
Ponatinib
Brand/Trade Names: Iclusig
Formula: C29H27F3N6O
Manufacturers: Hetero Drugs Limited, Mylan Inc, ARIAD Pharmaceuticals
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2012. Used for treatment of acute lymphoblastic leukemia and chronic myelogenous leukemia.
Pralsetinib
Brand/Trade Names: Gavreto
Formula: C27H32FN9O2
Manufacturer: Blueprint Medicines Corporation
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class:
Administration: Oral
Notes: First approved by the FDA in 2020 for treatment of non-small lung cancer.
Lenvatinib
Brand/Trade Names: Lenvima
Formula: C21H19ClN4O4
Manufacturers: Eisai Inc., Hangzhou Longshine Bio-Tech Co., Haoyuan Chemexpress Co.. MSN Laboratories Pvt Ltd
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I½
Administration: Oral
Notes: Approved by the FDA in 2015. Used for treatment of hepatocellular carcinoma, renal cell carcinoma, and thyroid cancer.
Neratinib
Brand/Trade Names: Nerlynx
Formula: C30H29ClN6O3
Manufacturers: Puma Biotechnology, Guangzhou Tosun Pharmaceutical, Hetero Drugs Limited, MSN Laboratories Pvt Ltd
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: Approved by the FDA in 2017. Approved for treatment of breast cancer.
Regorafenib
Brand/Trade Names: Stivarga
Formula: C21H17ClF4N4O4
Manufacturers: Bayer HealthCare Pharmaceuticals Inc., Hetero Drugs Limited, MSN Laboratories Pvt Ltd, Mylan Inc
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: Approved by the FDA in 2012. Angiogenesis inhibitor. Has been found to target at 14 different kinase enzymes. Used for treatment of colorectal cancer, gastrointestinal stromal tumor, and hepatocellular carcinoma.
Ripretinib
Brand/Trade Names: Qinlock
Formula: C24H21BrFN5O2
Manufacturer: Deciphera Pharmaceuticals, Inc
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: First approved by the FDA in 2020 for treatment of gastrointestinal-stromal tumors.
Selpercatinib
Brand/Trade Names: Retevmo
Formula: C29H31N7O3
Manufacturer: Loxo Oncology
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class:
Administration: Oral
Notes: First approved by the FDA in 2020 for treatment of thyroid cancer and non-small cell lung cancer.
Tivozanib
Brand/Trade Names: Fotivda
Formula: C22H19ClN4O5
Manufacturer: Avio Pharmaceuticals
Mechanism: Kinase Inhibitor
Protein substrate:
Class: Type II
Administration: Oral
Notes: First approved by the FDA in 2021 for treatment of renal cancer carcinoma.
Vandetanib
Brand/Trade Names: Caprelsa
Formula: C22H24BrFN4O2
Manufacturers: AstraZeneca Pharmaceuticals LP, Epoch Labs, Genzyme Corporation, Biotechnica Pharma Global
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2011. EGFR and VEGFR inhibitor. Has antiangiogenesis properties. Used for treatment of medullary thyroid cancer.
Ziv-aflibercept
Brand/Trade Names: Zaltrap
Formula: C4318H6788N1164O1304S32
Manufacturers: KinBio, Geneway Bio-Technology
Mechanism: VEGF inhibitor
Class: Fusion protein
Administration: Intravenous
Notes: Approved by the FDA in 2012. Angiogenesis inhibitor. Approved for treatment of colorectal cancer.
Venetoclax
Brand/Trade Names: Venclexta
Formula: C45H50ClN7O7S
Manufacturers: Alembic Pharmaceuticals Limited, Changzhou Pharmaceutical Factory, Hangzhou Longshine Bio-Tech Co., Hetero Drugs Limited
Mechanism: BCL-2 Inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: Approved by the FDA in 2016. Used for treatment of acute myeloid leukemia and chronic lymphocytic leukemia. Article from CLL Society
Dasatinib
Brand/Trade Names: Sprycel
Formula: C22H26ClN7O2S
Manufacturers: Apotex Pharmachem Inc, ALP Pharm, Acebright India Pharma Private Limited, Alembic Pharmaceuticals Limited, Apotex Pharmachem Inc.
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2006. Used for treatment of acute myeloid leukemia and chronic lymphocytic leukemia.
Erlotinib
Brand/Trade Names: Tarceva
Formula: C22H23N3O4
Manufacturers: Sun Pharmaceutical Industries, Acebright India Pharma Private Limited, Aspen Biopharma Labs Pvt Ltd, Beijing Lunarsun Pharmaceutical Co.
Mechanism: EGFR inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2004. Used for treatment of non smell-dell lung cancer and pancreatic cancer.
Erdafitinib
Brand/Trade Names: Balversa
Formula: C25H30N5O2
Manufacturers: Omgene Life Sciences, Janssen Products LP
Mechanism: FGFR inhibitor
Protein substrate: Tyrosine
Class: Type I½
Administration: Oral
Notes: Approved by the FDA in 2019. Approved for bladder (urothelial) carcinoma.
Futibatinib
Brand/Trade Names: Lytgobi
Formula: C22H22N6O3
Manufacturers: Taiho Oncology
Mechanism: FGFR inhibitor
Protein substrate: Tyrosine
Class:
Administration: Oral
Notes: Approved by the FDA in 2022. Approved for intrahepatic cholangiocarcinoma.
Gefitinib
Brand/Trade Names: Iressa
Formula: C22H24ClFN4O3
Manufacturers: Zuventus Healthcare Ltd, Acebright India Pharma Private Limited, Alembic Pharmaceuticals Limited, BDR Pharmaceuticals, Biotechnica Pharma Global
Mechanism: EGFR inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2003. Used for treatment of non-small cell lung cancer. Not used as often as it once was, as newer drugs have displaced it. More on gefitinib.
Imatinib
Brand/Trade Names: Gleevec, Glivec
Formula: C29H31N7O
Manufacturers: Lupin Pharmaceuticals, Acebright India Pharma Private Limited, Angels Pharma India Private Limited, Anhui HaiKang Pharmaceutical Co.
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: Approved by the FDA in 2001. Used for treatment of chronic eosinophilic leukemia, hypereosinophilic syndrome, chronic myelogenous leukemia, dermatofibrosarcoma protuberans. gastrointestinal stromal tumor, myelodysplastic/myeloproliferative neoplasms, and systemic mastocytosis. The introduction of imatinib to the market in 2001 is today considered historically significant as it was the first small molecule kinase inhibitor to be used in the clinic against cancer.
Lapatinib
Brand/Trade Names: Tykerb, Tyverb
Formula: C29H26ClFN4O4S
Manufacturers: Novartis Pharmaceuticals Corporation, Cambrex Corporation, ChemWerth Inc, Chengda Pharmaceuticals
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I½
Administration: Oral
Notes: Approved by the FDA in 2007. Used to treat advanced breast cancer, often after other medicines have been tried. EGFR inhibitor and HER2 inhibitor.
Nilotinib
Brand/Trade Names: Tasigna
Formula: C28H22F3N7O
Manufacturers: Novartis Pharmaceuticals Corporation, Acebright India Pharma Private Limited, Biotechnica Pharma Global, Biocon Limited, ChemWerth Inc
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type II
Administration: Oral
Notes: Approved by the FDA in 2007. Used to treat chronic myelogenous leukemia. More on nilotinib.
Pazopanib
Brand/Trade Names: Votrient
Formula: C21H23N7O2S
Manufacturers: Novartis Pharmaceuticals Corporation, Glaxo SmithKline Pharmaceuticals Ltd
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2009. Used for treatment of renal cell carcinoma and soft tissue sarcoma. Angiogenesis inhibitor. More.
Pemigatinib
Brand/Trade Names: Pemazyre
Formula: C24H27F2N5O4
Manufacturer: Incyte Corp
Mechanism: FGFR2 Kinase Inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: First approved by the FDA in 2020 for treatment of cholangiocarcinoma.
Ruxolitinib
Brand/Trade Names: Jakafi
Formula: C17H18N6
Manufacturers: Incyte Corporation, Hangzhou Longshine Bio-Tech Co., Seqens, Novartis India Ltd
Mechanism: Kinase Inhibitor, JAK Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2011. Used for treatment of myelofibrosis and polycythemia vera.
Sorafenib
Brand/Trade Names: Nexavar
Formula: C21H16ClF3N4O3
Manufacturers: Bayer HealthCare Pharmaceuticals Inc., Acebright India Pharma Private Limited, Alembic Pharmaceuticals Limited, Anhui HaiKang Pharmaceutical Co. Ltd, Aspire Lifesciences Pvt Ltd
Mechanism: Kinase Inhibitor
Protein substrate: Serine/threonine
Class: Type II
Administration: Oral
Notes: Angiogenesis inhibitor. Approved by the FDA in 2005. Used for treatment of hepatocellular carcinoma, renal cell carcinoma, and thyroid cancer.
Sunitinib
Brand/Trade Names: Sutent
Formula: C22H27FN4O2
Manufacturers: Pfizer, Acebright India Pharma Private Limited, Beijing Lunarsun Pharmaceutical Co., Biotechnica Pharma Global
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2006. Angiogenesis inhibitor. Employed against several hard-to-treat cancers. Used for treatment of gastrointestinal stromal tumor, pancreatic cancer, and renal cell carcinoma.
Tepotinib
Brand/Trade Names: Tepmetko
Formula: C29H28N6O2
Manufacturer: Merck
Mechanism: Kinase Inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: First approved by the FDA in 2021 for treatment of non-small cell lung cancer.
Tucatinib
Brand/Trade Names: Tukysa
Formula: C26H24N8O2
Manufacturer: Seattle Genetics, Shanghai Hope Chem
Mechanism: Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: First approved by the FDA in 2020 for treatment of metastatic breast cancer.
Larotrectinib
Brand/Trade Names: Vitrakvi
Formula: C21H22F2N6O2
Manufacturers: Loxo Oncology, Changzhou Pharmaceutical Factory, Hunan Huateng Pharmaceutical Co, Shandong Haohong Biotechnology Co., Mylan Inc
Mechanism: Tropomyosin kinase inhibitor
Protein substrate: tropomyosin
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2018 for treatment of soft tissue cancer that harbor NTRK fusions. “Tissue-agnostic” – meaning it can be labeled for tumors in general rather than for one type of cancer.
Bosutinib
Brand/Trade Names: Bosulif
Formula: C26H29Cl2N5O3
Manufacturers: ALP Pharm, Alembic Pharmaceuticals Limited, Hetero Drugs Limited, Hunan Huateng Pharmaceutical Co
Mechanism: kinase inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2012. More on bosutinib. Approved for treatment of chronic myelogenous leukemia.
Sotorasib
Brand/Trade Names: Lumakras
Formula: C30H30F2N6O3
Manufacturers: Amgen
Mechanism: KRAS kinase inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: Approved by the FDA in 2021. First KRAS inhibitor approved for cancer treatment. Approved for treatment of non small-cell lung cancer.
FLT3 inhibitors
Gilteritinib
Brand/Trade Names: Xospata
Formula: C29H24N8O3
Manufacturers: Astellas Pharma US, Hangzhou Longshine Bio-Tech Co.
Mechanism: FLT3 Kinase Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2018. Approved for treatment of acute myeloid leukemia.
Midostaurin
Brand/Trade Names: Rydapt
Formula: C35H30N4O4
Manufacturers: Novartis Pharmaceuticals Corporation, BrightGene Bio-Medical Technology Co., ChemWerth Inc, Chunghwa Chemical Synthesis & Biotech, Concord Biotech
Mechanism: FLT3 inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2017. Approved for treatment of acute myeloid leukemia, systemic mastocytosis, and mast cell leukemia.
Pacritinib
Brand/Trade Names: Vonjo
Formula: C28H32N4O3
Manufacturers:
Mechanism: FLT3 inhibitor and JAK inhibitor
Protein substrate: Tyrosine
Class:
Administration: Oral
Notes: Approved by the FDA in 2022. Approved for treatment of myelofibrosis.
Proteasome inhibitors
Bortezomib
Brand/Trade Names: Velcade
Formula: C19H25BN4O4
Manufacturers: Synthon s.r.o., Apicore LLC, Aspen Biopharma Labs Pvt Ltd, Aspire Lifesciences Pvt Ltd
Mechanism: proteasome inhibitor
Administration: Intravenous
Notes: The first approved proteasome inhibitor for cancer treatment, it has a boron atom in its molecule. Approved by the FDA in 2003. Used for treatment of mantle cell lymphoma and multiple myeloma.
Carfilzomib
Brand/Trade Names: Kyprolis
Formula: C40H57N5O7
Manufacturers: Biocon Limited, Biophore India Pharmaceuticals Pvt Ltd, Chongqing Pharmaceutical Research Institute Co Ltd, Chunghwa Chemical Synthesis & Biotech
Mechanism: proteasome inhibitor
Administration: Intravenous
Notes: Derivative of epoxomicin, which is extracted from bacteria. Approved by the FDA in 2012. Used for treatment of multiple myeloma.
Ixazomib
Brand/Trade Names: Ninlaro
Formula: C14H19Cl2N2O4
Manufacturers: Millennium Pharmaceuticals, Hangzhou Longshine Bio-Tech Co., Hunan Huateng Pharmaceutical Co
Mechanism: proteosome inhibitor
Administration: Oral
Notes: Approved by the FDA in 2015. Approved for treatment of multiple myeloma.
BTK Inhibitors
Pirtobrutinib
Brand/Trade Names: Jaypirca
Formula: C25H21F4N5O3
Manufacturers: Eli Lilly
Mechanism: Bruton’s tyrosine kinase inhibitor
Protein substrate:
Class:
Administration: Oral
Notes: Approved by the FDA in 2023 for treatment of mantle cell lymphoma
Ibrutinib
Brand/Trade Names: Imbruvica
Formula: C25H24N6O2
Manufacturers: Pharmacyclics LLC, Acebright India Pharma Private Limited, Alembic Pharmaceuticals Limited, Anhui HaiKang Pharmaceutical Co. Ltd
Mechanism: Bruton’s tyrosine kinase inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent, Type I
Administration: Oral
Notes: Approved by the FDA in 2013. Used for treatment of Waldenström macroglobulinemia, marginal zone lymphoma, mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma.
Acalabrutinib
Brand/Trade Names: Calquence
Formula: C26H23N7O2
Manufacturers: Cipla, Hangzhou Longshine Bio-Tech Co., Teva API, AstraZeneca Pharmaceuticals LP
Mechanism: Bruton’s tyrosine kinase inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: Approved by the FDA in 2017. “Acalabrutinib is a more highly specific BTK inhibitor than ibrutinib with fewer “off-target” effects, possibly accounting for an improved safety profile.” Used for treatment of mantle cell carcinoma and chronic lymphocytic leukemia.
Zanubrutinib
Brand/Trade Names: Brukinsa
Formula: C27H29N5O3
Manufacturer: BeiGene
Mechanism: Bruton’s tyrosine kinase inhibitor
Protein substrate: Tyrosine
Class: Type V – covalent
Administration: Oral
Notes: Approved by the FDA in 2019. Used for treatment of mantle cell lymphoma.
CDK Inhibitors
Ribociclib
Brand/Trade Names: Kisqali
Formula: C23H30N8O
Manufacturers: Changzhou Pharmaceutical Factory, Hetero Drugs Limited, Novartis Pharmaceuticals Corporation
Mechanism: Cyclin-dependent kinase inhibitor
Protein substrate: Serine/Threonine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2018. First drug approved under FDA’s Real-Time Oncology Review. Used for treatment of breast cancer.
Palbociclib
Brand/Trade Names: Ibrance
Formula: C24H29N7O2
Manufacturers: U.S. Pharmaceuticals, Acebright India Pharma Private Limited, Alembic Pharmaceuticals Limited, Apotex Pharmachem Inc., Beijing Lunarsun Pharmaceutical Co.
Mechanism: Cyclin-dependent kinase inhibitor
Protein substrate: Serine/Threonine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2015. Used for treatment of breast cancer.
Abemaciclib
Brand/Trade Names: Verzenio
Formula: C27H32F2N8
Manufacturers: Biophore India Pharmaceuticals Pvt Ltd, Johnson Matthey PLC, MSN Laboratories Pvt Ltd, Eli Lilly and Company
Mechanism: Cyclin-dependant kinase inhibitor
Protein substrate: Serine/Threonine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2017. Approved for treatment of breast cancer.
BRAF Inhibitors
Vemurafenib
Brand/Trade Names: Zelboraf
Formula: C23H18ClF2N3O3S
Manufacturers: Biotechnica Pharma Global, Epoch Labs, Fermion Oy, Hetero Drugs Limited
Mechanism: B-Raf enzyme inhibitor
Protein substrate: Serine/Threonine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2011. Has a greater affinity for mutant form of the B-Raf kinase than for wild-type B-Raf. Approved for treatment of Erdheim-Chester disease and melanoma.
Encorafenib
Brand/Trade Names: Braftovi
Formula: C22H27ClFN7O4S
Manufacturer: Array BioPharma Inc.
Mechanism: BRAF Inhibitor
Protein substrate: Serine/Threonine
Class: Type I
Administration: Intravenous
Notes: Approved by the FDA in 2018. Approved for treatment of melanoma.
Dabrafenib
Brand/Trade Names: Tafinlar
Formula: C23H20F3N5O2S2
Manufacturers: Guangdong Raffles PharmaTech Co Ltd, Hangzhou Longshine Bio-Tech Co., Shenzhen HwaGen Pharmaceutical, Novartis Pharmaceuticals Corporation
Mechanism: BRAF Inhibitor
Protein substrate: Serine/threonine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2013. Approved for treatment of anaplastic thyroid cancer, melanoma, and non-small cell lung cancer,
MEK Inhibitors
Medicines that inhibit mitogen-activated protein kinase kinase enzymes
Trametinib
Brand/Trade Names: Mekinist
Formula: C26H23FIN5O4
Manufacturers: Novartis Pharmaceuticals Corporation Hangzhou Longshine Bio-Tech Co., MSN Laboratories Pvt Ltd, Mylan Inc, Shanghai Hope Chem
Mechanism: MEK1 and MEK2 inhibitor
Protein substrate:
Class: Type III
Administration: Oral
Notes: Approved to treat BRAF-mutated melanoma. Approved by the FDA in 2013. Approved for treatment of anaplastic thyroid cancer, melanoma, and non-small cell lung cancer.
Cobimetinib
Brand/Trade Names: Cotellic
Formula: C21H21F3IN3O2
Manufacturer: Genentech (Roche)
Mechanism: MEK inhibitor
Protein substrate:
Class: Type III
Administration: Oral
Notes: Approved by the FDA in 2015. Given in combination with vemurafenib. Approved for treatment of melanoma.
Binimetinib
Brand/Trade Names: Mektovi
Formula: C17H15BrF2N4O3
Manufacturers: Omgene Life Sciences, Array BioPharma Inc.
Mechanism: MEK Inhibitor
Protein substrate:
Class: Type III
Administration: Oral
Notes: Approved by the FDA in 2018 for treatment of melanoma.
ALK Inhibitors
Medicines that inhibit receptors of tyrosine kinase anaplastic lymphoma kinase (ALK),
Crizotinib
Brand/Trade Names: Xalkori
Formula: C21H22Cl2FN5O
Manufacturers: Pfizer Laboratories Div Pfizer Inc, Apothecon Pharmaceuticals, DEAFARMA, Danesh Kimia Pharmed
Mechanism: ALK Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2011. Used for treatment of non-small cell lung cancer.
Ceritinib
Brand/Trade Names: Zykadia
Formula: C28H36ClN5O3S
Manufacturers: Novartis Pharmaceuticals Corporation, Hetero Drugs Limited, MSN Laboratories Pvt Ltd, Natco Pharma Limited
Mechanism: ALK Inhibitor
Protein substrate: Tryosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2014 for treatment of non-small cell lung cancer.
Alectinib
Brand/Trade Names: Alecensa
Formula: C30H34N4O2
Manufacturers: Hunan Huateng Pharmaceutical Co, Shandong Haohong Biotechnology Co., Shanghai Hope Chem
Mechanism: ALK Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2015 for treatment of non-small cell lung cancer.
Brigatinib
Brand/Trade Names: Alunbrig
Formula: C29H39ClN7O2P
Manufacturers: Mylan Inc, Shandong Haohong Biotechnology Co., Shanghai Hope Chem, Millennium Pharmaceuticals, Inc
Mechanism: ALK Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2017 for treatment of non-small cell lung cancer.
Lorlatinib
Brand/Trade Names: Lorbrena
Formula: C23H20OFN5O2
Manufacturers: Pfizer Laboratories Div Pfizer Inc, Shanghai Hope Chem, Teva API
Mechanism: ALK Inhibitor
Protein substrate: Tyrosine
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2018. Used for treatment of non-small cell lung cancer.
PI3K Inhibitors
Copanlisib
Brand/Trade Names: Aliqopa
Formula: C23H28N8O4
Manufacturers: Sun-shine Chem, Bayer HealthCare Pharmaceuticals Inc.
Mechanism: PI3K Inhibitor
Protein substrate:
Class: Type I½
Administration: Intravenous
Notes: Approved by the FDA in 2017 for treatment of follicular lymphoma.
Duvelisib
Brand/Trade Names: Copiktra
Formula: C22H17ClN6O
Manufacturers: Epoch Labs, Verastem
Mechanism: PI3K Inhibitor
Protein substrate:
Class: Type I
Administration: Intravenous
Notes: Approved by the FDA in 2018. Approved for treatment of follicular lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma.
Alpelisib
Brand/Trade Names: Piqray
Formula: C19H22F3N5O2S
Manufacturers: ScinoPharm Taiwan, Novartis Pharmaceuticals Corporation
Mechanism: PI3K Inhibitor
Protein substrate:
Class: Type I½
Administration: Oral
Notes: Approved by the FDA in 2019 for treatment of breast cancer.
Idelalisib
Brand/Trade Names: Zydelig
Formula: C22H18FN7O
Manufacturers: Gilead Sciences, Haoyuan Chemexpress Co, Hetero Drugs Limited, Lupin Ltd
Mechanism: Phosphatidylinositol 3-kinase inhibitor or phosphoinositide 3-kinase inhibitor
Protein substrate:
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2014. Approved for treatment of chronic lymphocytic leukemia and non-Hodgkin’s lymphoma.
Umbralisib
Brand/Trade Names: Ukoniq
Formula: C31H24F3N5O3
Manufacturer: TG Therapeutics, Inc
Mechanism: PI3K inhibitor
Protein substrate:
Class: Type I
Administration: Oral
Notes: Approved by the FDA in 2021. Approved for treatment of lymphoma.
Hedgehog signaling pathway inhibitors
Glasdegib
Brand/Trade Names: Daurismo
Formula: C21H22N6O
Manufacturer: Pfizer Laboratories
Mechanism: Hedgehog signaling pathway inhibitor
Administration: Oral
Notes: Approved by the FDA in 2018. Approved for treatment of acute myeloid leukemia.
Sonidegib
Brand/Trade Names: Odomzo
Formula: C26H26F3N3O3
Manufacturers: Hangzhou DayangChem Co., Sun Pharmaceutical Industries, Inc.
Mechanism: Hedgehog signaling pathway inhibitor
Administration: Oral
Notes: Approved by FDA in 2015. Approved for treatment of basal cell carcinoma.
Vismodegib
Brand/Trade Names: Erivedge
Formula: C19H14Cl2N2O3S
Manufacturers: DEAFARMA, Hetero Drugs Limited, Omgene Life Sciences
Mechanism: Hedgehog pathway inhibitor
Administration: Oral
Notes: Approved by the FDA in 2012. Used for treatment of basal cell carcinoma.