Inhibitor Drugs

Afatinib

Brand/Trade Names: Gilotrif

Formula: C24H25ClFN5O3

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes: EGFR inhibitor

Axitinib

Brand/Trade Names: Inlyta

Formula: C22H18N4Osub>S

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes: VEGF inhibitor and angiogenesis inhibitor.

Cabozantinib

Brand/Trade Names: Cometriq

Formula: C28H24FN3O5

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes:

Dacomitinib

Brand/Trade Names: Vizimpro

Formula:

C24H25ClFN5O2

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes:

Osimertinib

Brand/Trade Names: Tagrisso, Mereletinib

Formula: C28H33N7O2

Mechanism: tyrosine kinase inhibitor

Class:

Administration: Oral

Notes: EGFR inhibitor

Ponatinib

Brand/Trade Names: Iclusig

Formula: C29H27F3N6O

Mechanism: tyrosine kinase inhibitor

Class:

Administration: Oral

Notes:

Lenvatinib

Brand/Trade Names: Lenvima

Formula: C21H19ClN4O4

Mechanism: tyrosine kinase inhibitor

Class:

Administration: Oral

Notes:

Neratinib

Brand/Trade Names: Neratinib

Formula: C30H29ClN6O3

Mechanism: tyrosine kinase inhibitor

Class:

Administration: Oral

Notes:

Regorafenib

Brand/Trade Names: Stivarga

Formula: C21H17ClF4N4O4

Mechanism: tyrosine kinase inhibitor

Class:

Administration: Oral

Notes:

Vandetanib

Brand/Trade Names: Caprelsa

Formula: C22H24BrFN4O2

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes: EGFR and VEGFR inhibitor

Ziv-aflibercept

Brand/Trade Names: Zaltrap

Formula: C4318H6788N1164O1304S32

Mechanism: VEGF inhibitor

Class: MAB

Administration: Intraveneous

Notes:

Venetoclax

Brand/Trade Names: Venclexta

Formula: C45H50ClN7O7S

Mechanism: BCL-2 Inhibitor

Class:

Administration: Oral

Notes:  Article from CLL Society

Dasatinib

Brand/Trade Names: Sprycel

Formula: C22H26ClN7O2S

Mechanism: Tyrosine Kinase Inhibitor

Class:

Administration: Oral

Notes: Pretty much used only to treat leukemia.

Erlotinib

Brand/Trade Names: Tarceva

Formula: C22H23N3O4

Mechanism: EGFR inhibitor

Class:

Administration: Oral

Notes:

Gefitinib

Brand/Trade Names: Iressa

Formula: C22H24ClFN4O3

Mechanism: EGFR inhibitor

Class:

Administration: Oral

Notes: 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:

Class:

Administration: Oral

Notes: Blocks the protein made by the bcr/abl oncogene

Lapatinib

Brand/Trade Names: Tykerb, Tyverb

Formula: C29H26ClFN4O4S

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: Used against advanced breast cancer, often after other medicines have been tried.

Nilotinib

Brand/Trade Names: Tasigna

Formula: C28H22F3N7O

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: FDA-approved to treat chronic myelogenous leukemia. More on nilotinib.

Pazopanib

Brand/Trade Names: Votrient

Formula: C21H23N7O2S

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: Approved for advanced renal cell carcinoma. Can cause liver damage. More.

Ruxolitinib

Brand/Trade Names: Jakafi

Formula: C17H18N6

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: Approved for advanced renal cell carcinoma. Can cause liver damage. More.

Sorafenib

Brand/Trade Names: Nexavar

Formula: C21H16ClF3N4O3

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: Approved for certain types of liver and kidney cancer.

Sunitinib

Brand/Trade Names: Sutent

Formula: C22H27FN4O2

Mechanism: Kinase Inhibitor

Class:

Administration: Oral

Notes: Employed against several hard-to-treat cancers.

FLT3 inhibitors

Midostaurin

Brand/Trade Names: Rydapt

Formula: C35H30N4O4

Mechanism: FLT3 inhibitor

Class:

Administration: Oral

Notes:

Proteasome inhibitors

Bortezomib

Brand/Trade Names: Velcade

Formula: C19H25BN4O4

Mechanism: proteasome inhibitor

Class:

Administration: Intraveneous

Notes: The first approved proteasome inhibitor for cancer treatment, it has a boron atom in its molecule.

Carfilzomib

Brand/Trade Names: Kyprolis

Formula: C40H57N5O7

Mechanism: proteasome inhibitor

Class:

Administration: Intraveneous

Notes: Derivative of epoxomicin, which is extracted from bacteria.

Ixazomib

Brand/Trade Names: Ninlaro

Formula: C14H19Cl2N2O4

Mechanism: proteosome inhibitor

Class:

Administration: Oral

Notes: Molecule contains a boron atom

 

BTK Inhibitors

Ibrutinib

Brand/Trade Names: Imbruvica

Formula: C25H24N6O2

Mechanism: Bruton’s tyrosine kinase inhibitor

Class:

Administration: Oral

Notes:

Acalabrutinib

Brand/Trade Names: Calquence

Formula: C26H23N7O2

Mechanism: Bruton’s tyrosine kinase inhibitor

Class:

Administration: Oral

Notes: “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

Class:

Administration: Oral

Notes: “Indicated in combination with an aromatase inhibitor (eg, letrozole) for the treatment of pre/perimenopausal or postmenopausal women…as initial endocrine-based therapy”

Palbociclib

Brand/Trade Names: Ibrance

Formula: C24H29N7O2

Mechanism: Cyclin-dependent kinase inhibitor

Class:

Administration: Oral

Notes:

Abemaciclib

Brand/Trade Names: Verzenio

Formula: C27H32F2N8

Mechanism: Cyclin-dependent kinase inhibitor

Class:

Administration: Oral

Notes:

BRAF Inhibitors

Vemurafenib

Brand/Trade Names: Zelboraf

Formula: C23H18ClF2N3O3S

Mechanism: B-Raf enzyme inhibitor

Class:

Administration: Oral

Notes:

Encorafenib

Brand/Trade Names: Braftovi

Formula: C22H27ClFN7O4S

Mechanism: BRAF Inhibitor

Class:

Administration: Intraveneous

Notes:

Dabrafenib

Brand/Trade Names: Tafinlar

Formula: C23H20F3N5O2S2

Mechanism: BRAF Inhibitor

Class:

Administration: Oral

Notes:

MEK Inhibitors

Medicines that inhibit mitogen-activated protein kinase kinase enzymes

Trametinib

Brand/Trade Names: Mekinist

Formula: C26H23FIN5O4

Mechanism: MEK1 and MEK2 inhibitor

Class:

Administration: Oral

Notes: Approved to treat BRAF-mutated melanoma

Cobimetinib

Brand/Trade Names: Cotellic

Formula: C21H21F3IN3O2

Mechanism: MEK inhibitor

Class:

Administration: Oral

Notes: Given in combination with vemurafenib

Binimetinib

Brand/Trade Names: Mektovi

Formula: C17H15BrF2N4O3

Mechanism: MEK Inhibitor

Class:

Administration: Oral

Notes:

ALK Inhibitors

Medicines that inhibit receptors of tyrosine kinase anaplastic lymphoma kinase (ALK),

Crizotinib

Brand/Trade Names: Xalkori

Formula: C21H22Cl2FN5O

Mechanism: ALK Inhibitor

Class:

Administration: Oral

Notes:

Ceritinib

Brand/Trade Names: Zykadia

Formula: C28H36ClN5O3S

Mechanism: ALK Inhibitor

Class:

Administration: Oral

Notes:

Alectinib

Brand/Trade Names: Alecensa

Formula: C30H34N4O2

Mechanism: ALK Inhibitor

Class:

Administration: Oral

Notes:

Brigatinib

Brand/Trade Names: Alunbrig

Formula: C29H39ClN7O2P

Mechanism: ALK Inhibitor

Class:

Administration: Oral

Notes:

 

P1K3 Inhibitors

Copanlisib

Brand/Trade Names: Aliqopa

Formula: C23H28N8O4

Mechanism: PIK3 Inhibitor

Class:

Administration: Intraveneous

Notes:

Duvelisib

Brand/Trade Names: Copiktra

Formula: C22H17ClN6O

Mechanism: PIK3 Inhibitor

Class:

Administration: Intraveneous

Notes:

Idelalisib

Brand/Trade Names: Zydelig

Formula: C22H18FN7O

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

Class:

Administration: Oral

Notes:

 

Hedgehog signaling pathway inhibitors

Sonidegib

Brand/Trade Names: Odomzo

Formula: C26H26F3N3O3

Mechanism: Hedgehog signaling pathway inhibitor

Class:

Administration: Oral

Notes:

Vismodegib

Brand/Trade Names: Erivedge

Formula: C19H14Cl2N2O3S

Mechanism: Hedgehog pathway inhibitor

Class:

Administration: Oral

Notes: 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: 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: