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.