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.

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.

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. 

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.

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.

Ponatinib

Brand/Trade Names: Iclusig

Formula: C29H27F3N6O

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2012. 

Lenvatinib

Brand/Trade Names: Lenvima

Formula: C21H19ClN4O4

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2015.

Neratinib

Brand/Trade Names: Nerlynx

Formula: C30H29ClN6O3

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.

Regorafenib

Brand/Trade Names: Stivarga

Formula: C21H17ClF4N4O4

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2012.  Has been found to target at 14 different kinase enzymes

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.

Ziv-aflibercept

Brand/Trade Names: Zaltrap

Formula: C4318H6788N1164O1304S32

Mechanism: VEGF inhibitor

Protein substrate:

Class: MAB

Administration: Intravenous

Notes:  Approved by the FDA in 2012.

Venetoclax

Brand/Trade Names: Venclexta

Formula: C45H50ClN7O7S

Mechanism: BCL-2 Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2016. 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.

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 to pancreatic cancer for 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.

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.  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.

Gilteritinib

Brand/Trade Names: Xospata

Formula: C29H24N8O3

Mechanism: Kinase Inhibitor

Protein substrate:

Class:  Type II

Administration: Oral

Notes: Approved by the FDA in 2018.

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 advanced renal cell carcinoma. Can cause liver damage. More.

Ruxolitinib

Brand/Trade Names: Jakafi

Formula: C17H18N6

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class: Type I

Administration: Oral

Notes: First approved by the FDA in 2011.  Approved for advanced renal cell carcinoma. Can cause liver damage. More.

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.  First approved by the FDA in 2005.

Sunitinib

Brand/Trade Names: Sutent

Formula: C22H27FN4O2

Mechanism: Kinase Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes: First approved by the FDA in 2006.  Employed against several hard-to-treat cancers.

Larotrectinib

Brand/Trade Names: Vitrakvi

Formula: C21H22F2N6O2

Mechanism: Tropomyosin kinase inhibitor

Protein substrate:  tropomyosin

Class:

Administration: Oral

Notes: Approved by the FDA in 2018.  “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.

FLT3 inhibitors

Midostaurin

Brand/Trade Names: Rydapt

Formula: C35H30N4O4

Mechanism: FLT3 inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.

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.

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.

Ixazomib

Brand/Trade Names: Ninlaro

Formula: C14H19Cl2N2O4

Mechanism: proteosome inhibitor

Class:

Administration: Oral

Notes: Approved by the FDA in 2015.

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.

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.”

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.

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.

Abemaciclib

Brand/Trade Names: Verzenio

Formula: C27H32F2N8

Mechanism: Cyclin-dependant kinase inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.

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.

Encorafenib

Brand/Trade Names: Braftovi

Formula: C22H27ClFN7O4S

Mechanism: BRAF Inhibitor

Protein substrate:

Class:

Administration: Intravenous

Notes:  Approved by the FDA in 2018.

Dabrafenib

Brand/Trade Names: Tafinlar

Formula: C23H20F3N5O2S2

Mechanism: BRAF Inhibitor

Protein substrate: Serine/threonine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2013.

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.

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.

Binimetinib

Brand/Trade Names: Mektovi

Formula: C17H15BrF2N4O3

Mechanism: MEK Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes:  Approved by the FDA in 2018.

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.

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.

Alectinib

Brand/Trade Names: Alecensa

Formula: C30H34N4O2

Mechanism: ALK Inhibitor

Protein substrate: Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA  in 2015.

Brigatinib

Brand/Trade Names: Alunbrig

Formula: C29H39ClN7O2P

Mechanism: ALK Inhibitor

Protein substrate:  Tyrosine

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017.

Lorlatinib

Brand/Trade Names: Lorbrena

Formula: C23H20OFN5O2

Mechanism: ALK Inhibitor

Protein substrate:

Class:

Administration: Oral

Notes: First approved by the FDA in 2018.

P1K3 Inhibitors

Copanlisib

Brand/Trade Names: Aliqopa

Formula: C23H28N8O4

Mechanism: PIK3 Inhibitor

Protein substrate:

Class:

Administration: Intravenous

Notes:  Approved by the FDA in 2017.

Duvelisib

Brand/Trade Names: Copiktra

Formula: C22H17ClN6O

Mechanism: PIK3 Inhibitor

Protein substrate:

Class:

Administration: Intravenous

Notes:  Approved by the FDA in 2018.

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.

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.

Sonidegib

Brand/Trade Names: Odomzo

Formula: C26H26F3N3O3

Mechanism: Hedgehog signaling pathway inhibitor

Class:

Administration: Oral

Notes:  Approved by FDA  in 2015.

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

IDH inhibitors

Enasidenib

Brand/Trade Names: Idhifa

Formula: C19H17F6N7O

Mechanism: IDH2 inhibitor

Class:

Administration: Oral

Notes:  Approved by the FDA in 2017. Technology Review said “it has been hailed as the first real advance for the disease in 30 years”.

Ivosidenib

Brand/Trade Names: Tibsovo

Formula: C28H22ClF3N6O3

Mechanism: IDH1 inhibitor

Class:

Administration: Oral

Notes:  Approved by the FDA in 2018.