Inhibitor Drugs

Afatinib

Brand/Trade Names: Gilotrif

Formula: C24H25ClFN5O3

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.

Axitinib

Brand/Trade Names: Inlyta

Formula: C22H18N4OS

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:  Type II

Administration: Oral

Notes: First approved by the FDA in 2012.  VEGF inhibitor and angiogenesis inhibitor.  Approved for treatment of renal cell carcinoma.

Cabozantinib

Brand/Trade Names: Cometriq

Formula: C28H24FN3O5

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2012.   Angiogenesis inhibitor. Approved for treatment of renal cell carcinoma, hepatocellular carcinoma, and medullary thyroid cancer.

Dacomitinib

Brand/Trade Names: Vizimpro

Formula: C24H25ClFN5O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2018.  EGFR inhibitor and HER inhibitor.  Approved for treatment of non-small cell lung cancer.

Entrectinib

Brand/Trade Names: Rozlytrek

Formula: C31H34F2N6O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2019. Tumor-agnostic drug.

Osimertinib

Brand/Trade Names: Tagrisso, Mereletinib

Formula: C28H33N7O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type V – covalent

Administration: Oral

Notes: EGFR inhibitor.  Approved by the FDA in 2015.  Approved for treatment of non-small cell lung cancer.

Ponatinib

Brand/Trade Names: Iclusig

Formula: C29H27F3N6O

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2012.   Approved for treatment of acute lymphoblastic leukemia and chronic myelogenous leukemia.

Lenvatinib

Brand/Trade Names: Lenvima

Formula: C21H19ClN4O4

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2015.  Approved for treatment of hepatocellular carcinoma, renal cell carcinoma, and thyroid cancer.  Estimated sales of $540 million in 2018.

Neratinib

Brand/Trade Names: Nerlynx

Formula: C30H29ClN6O3

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.  Approved for treatment of breast cancer.

Regorafenib

Brand/Trade Names: Stivarga

Formula: C21H17ClF4N4O4

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2012.  Angiogenesis inhibtor. Has been found to target at 14 different kinase enzymes.  Approved for treatment of colorectal cancer, gastrointestinal stromal tumor, and hepatocellular carcinoma.

Vandetanib

Brand/Trade Names: Caprelsa

Formula: C22H24BrFN4O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2011.  EGFR and VEGFR inhibitor.  Has antiangiogenesis properties.  Approved for treatment of medullary thyroid cancer.

Ziv-aflibercept

Brand/Trade Names: Zaltrap

Formula: C4318H6788N1164O1304S32

Mechanism: VEGF inhibitor

Protein substrate:

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

Mechanism: BCL-2 Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2016 for treatment of acute myeloid leukemia and chronic lymphocytic leukemia. Article from CLL Society

Dasatinib

Brand/Trade Names: Sprycel

Formula: C22H26ClN7O2S

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2006.  Pretty much used only to treat leukemia.  Formally approved for treatment of acute myeloid leukemia and chronic lymphocytic leukemia.

Erlotinib

Brand/Trade Names: Tarceva

Formula: C22H23N3O4

Mechanism: EGFR inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  First approved by the FDA in 2004 for lung cancer.  Expanded approval for treatment of pancreatic cancer.

Erdafitinib

Brand/Trade Names: Balversa

Formula: C25H30N5O2

Mechanism: FGFR inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2019.  Approved for bladder (urothelial) carcinoma.

Gefitinib

Brand/Trade Names: Iressa

Formula: C22H24ClFN4O3

Mechanism: EGFR inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2003.  Approved 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

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:  Type II

Administration: Oral

Notes: First approved by the FDA in 2001.  Approved for treatment of chronic eosinophilic leukemia, hypereosinophilic syndrome, chronic myelogenous leukemia, dermatofibrosarcoma protuberans. gastrointestinal stromal tumor, myelodysplastic/myeloproliferative neoplasms, and systemic mastocytosis

Gilteritinib

Brand/Trade Names: Xospata

Formula: C29H24N8O3

Mechanism: Kinase Inhibitor

Protein substrate:

Class:  Type II

Administration: Oral

Notes: Approved by the FDA in 2018.  Approved for treatment of acute myeloid leukemia.

Lapatinib

Brand/Trade Names: Tykerb, Tyverb

Formula: C29H26ClFN4O4S

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2007.  Used against advanced breast cancer, often after other medicines have been tried.  EGFR inhbitor and HER2 inhbitor.

Nilotinib

Brand/Trade Names: Tasigna

Formula: C28H22F3N7O

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type III

Administration: Oral

Notes: First approved by the FDA in 2007.  Approved to treat chronic myelogenous leukemia. More on nilotinib.

Pazopanib

Brand/Trade Names: Votrient

Formula: C21H23N7O2S

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2009.  Approved for treatment of renal cell carcinoma and soft tissue sarcoma.  Angiogenesis inhibitor.  Approved for advanced renal cell carcinoma. Can cause liver damage. More.

Ruxolitinib

Brand/Trade Names: Jakafi

Formula: C17H18N6

Mechanism: Kinase Inhibitor, JAK Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2011.   Approved for treatment of myelofibrosis and polycythemia vera.  Estimated sales in 2018: $2.36 billion.

Sorafenib

Brand/Trade Names: Nexavar

Formula: C21H16ClF3N4O3

Mechanism: Kinase Inhibitor

Protein substrate: Serine/threonine

Class: Type II

Administration: Oral

Notes: Approved for certain types of liver and kidney cancer.  Angiogenesis inhibtor.  First approved by the FDA in 2005.  Approved for treatment of hepatocellular carcinoma, renal cell carcinoma, and thyroid cancer.

Sunitinib

Brand/Trade Names: Sutent

Formula: C22H27FN4O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2006.  Angiogensis inhibitor.  Employed against several hard-to-treat cancers.  Approved for gastrointestinal stromal tumor, pancreatic cancer, and renal cell carcinoma.

Larotrectinib

Brand/Trade Names: Vitrakvi

Formula: C21H22F2N6O2

Mechanism: Tropomyosin kinase inhibitor

Protein substrate:  tropomyosin

Class:

Administration: Oral

Notes: Approved by the FDA in 2018 for treatment of soft tissue.  “Tissue-agnostic” – meaning it can be labeled for solid tumors in general rather than for one type of cancer.

Bosutinib

Brand/Trade Names: Bosulif

Formula: C26H29Cl2N5O3

Mechanism: kinase inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: Approved by the FDA in 2012.  More on bosutinib. Approved for treatment of chronic myelogenous leukemia.

FLT3 inhibitors

Midostaurin

Brand/Trade Names: Rydapt

Formula: C35H30N4O4

Mechanism: FLT3 inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.  Approved for treatment of acute myeloid leukemia, systemic mastocytosis, and mast cell leukemia.

Proteasome inhibitors

Bortezomib

Brand/Trade Names: Velcade

Formula: C19H25BN4O4

Mechanism: proteasome inhibitor

Class:

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.  Approved for treatment of mantle cell lymphoma and multiple myeloma.

Carfilzomib

Brand/Trade Names: Kyprolis

Formula: C40H57N5O7

Mechanism: proteasome inhibitor

Class:

Administration: Intravenous

Notes: Derivative of epoxomicin, which is extracted from bacteria.  Approved by the FDA in 2012.   Approved for treatment of multiple myeloma.

Ixazomib

Brand/Trade Names: Ninlaro

Formula: C14H19Cl2N2O4

Mechanism: proteosome inhibitor

Class:

Administration: Oral

Notes: Approved by the FDA in 2015.   Approved for treatment of multiple myeloma.  Estimated sales of $590 million in 2018.

BTK Inhibitors

Ibrutinib

Brand/Trade Names: Imbruvica

Formula: C25H24N6O2

Mechanism: Bruton’s tyrosine kinase inhibitor

Protein substrate: Tyrosine

Class: Type V

Administration: Oral

Notes:  Approved by the FDA in 2013.   Approved for treatment of Waldenström macroglobulinemia, marginal zone lymphoma, mantle cell lymphoma, chronic lymphocytic leukemia, and small lymphocytic lymphoma.  Estimated sales in 2018 were $4.45 billion.

Acalabrutinib

Brand/Trade Names: Calquence

Formula: C26H23N7O2

Mechanism: Bruton’s tyrosine kinase inhibitor

Protein substrate:

Class:

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.” Approved for treatment of mantle cell carcinoma.

CDK Inhibitors

Ribociclib

Brand/Trade Names: Kisqali

Formula: C23H30N8O

Mechanism: Cyclin-dependent kinase inhibitor

Protein substrate: Serine/Threonine

Class:

Administration: Oral

Notes: Approved by the FDA in 2018. First drug approved under FDA’s Real-Time Oncology Review.  Approved for treatment of breast cancer.

Palbociclib

Brand/Trade Names: Ibrance

Formula: C24H29N7O2

Mechanism: Cyclin-dependant kinase inhibitor

Protein substrate: Serine/Threonine

Class:

Administration: Oral

Notes: Approved by the FDA in 2017.   Approved for treatment of breast cancer.   Estimated sales of $723 million in 2015.

Abemaciclib

Brand/Trade Names: Verzenio

Formula: C27H32F2N8

Mechanism: Cyclin-dependant kinase inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.  Approved for treatment of breast cancer.

BRAF Inhibitors

Vemurafenib

Brand/Trade Names: Zelboraf

Formula: C23H18ClF2N3O3S

Mechanism: B-Raf enzyme inhibitor

Protein substrate:

Class:

Administration: Oral

Notes: First 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

Mechanism: BRAF Inhibitor

Protein substrate:

Class:

Administration: Intravenous

Notes:  Approved by the FDA in 2018.  Approved for treatment of melanoma.

Dabrafenib

Brand/Trade Names: Tafinlar

Formula: C23H20F3N5O2S2

Mechanism: BRAF Inhibitor

Protein substrate: Serine/threonine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2013.  Approved for treatment of anaplastic thyroid cancer, melanoma, and non-small cell lung cancer.  Estimated sales of $1.16 billion in 2018.

MEK Inhibitors

Medicines that inhibit mitogen-activated protein kinase kinase enzymes

Trametinib

Brand/Trade Names: Mekinist

Formula: C26H23FIN5O4

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

Mechanism: MEK inhibitor

Protein substrate:

Class:

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

Mechanism: MEK Inhibitor

Protein substrate:

Class:

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

Mechanism: ALK Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2011 for treatment of non-small cell lung cancer.

Ceritinib

Brand/Trade Names: Zykadia

Formula: C28H36ClN5O3S

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

Mechanism: ALK Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA  in 2015 for treatment of non-small cell lung cancer.

Brigatinib

Brand/Trade Names: Alunbrig

Formula: C29H39ClN7O2P

Mechanism: ALK Inhibitor

Protein substrate:  Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017 for treatment of non-small cell lung cancer.

Lorlatinib

Brand/Trade Names: Lorbrena

Formula: C23H20OFN5O2

Mechanism: ALK Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes: First approved by the FDA in 2018 for treatment of non-small cell lung cancer.

PI3K Inhibitors

Copanlisib

Brand/Trade Names: Aliqopa

Formula: C23H28N8O4

Mechanism: PI3K Inhibitor

Protein substrate:

Class:

Administration: Intravenous

Notes:  Approved by the FDA in 2017 for treatment of follicular lymphoma.

Duvelisib

Brand/Trade Names: Copiktra

Formula: C22H17ClN6O

Mechanism: PI3K Inhibitor

Protein substrate:

Class:

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

Mechanism: PI3K Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2019 for treatment of breast cancer.

Idelalisib

Brand/Trade Names: Zydelig

Formula: C22H18FN7O

Mechanism: Phosphatidylinositol 3-kinase inhibitor or phosphoinositide 3-kinase inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2014.  Approved for treatment of chronic lymphocytic leukemia and non-Hodgkin’s lymphoma.

Hedgehog signaling pathway inhibitors

Glasdegib

Brand/Trade Names: Daurismo

Formula: C21H22N6O

Mechanism: Hedgehog signaling pathway inhibitor

Class:

Administration: Oral

Notes:  Approved by the FDA in 2018.  Approved for treatment of acute myeloid leukemia.

Sonidegib

Brand/Trade Names: Odomzo

Formula: C26H26F3N3O3

Mechanism: Hedgehog signaling pathway inhibitor

Class:

Administration: Oral

Notes:  Approved by FDA in 2015. Approved for treatment of basal cell carcinoma.

Vismodegib

Brand/Trade Names: Erivedge

Formula: C19H14Cl2N2O3S

Mechanism: Hedgehog pathway inhibitor

Class:

Administration: Oral

Notes: First approved by the FDA in 2012.  Large Trial Confirms Vismodegib Benefit in Basal Cell Carcinoma   Approved for treatment of basal cell carcinoma.

Selective inhibitors of nuclear export (SINE)

Selinexor

Brand/Trade Names: Xpovio

Formula: C17H11F6N7O

Mechanism: SINE

Class:

Administration: Oral

Notes: First approved by the FDA in 2019.  Large Trial Confirms Vismodegib Benefit in Basal Cell Carcinoma   Approved for treatment of multiple myeloma.