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. Author manuscript; available in PMC: 2023 Sep 28.
Published in final edited form as: J Med Chem. 2019 Oct 9;63(2):441–469. doi: 10.1021/acs.jmedchem.9b00640

Table 1:

Various approved chiral kinase inhibitors

Drug Name Tradename Approval Developer Target Indication
Sirolimus* RAPAMUNE® 199923 Wyeth-Ayerst Research FKBP12/mTOR Immunosuppressant
Temsirolimus* TORISEL® 200724 Wyeth Pharmaceuticals FKBP12/mTOR Advanced RCCa
Everolimus* AFINITOR® 2009 Novartis FKBP12/mTOR Immunosuppressant
Crizotinib XALKORI® 2011 Pfizer ALK, c-MET, HGFR NSCLC
Ruxolitinib JAKAFI® 2011 Incyte JAK1, JAK2 Myelofibrosis
Tofacitinib XELJANZ® 2012 Pfizer JAK2, JAK3 RAb
Afatinib GILOTRIF® 2013 Boehringer Ingelheim EGFR, HER2 NSCLCc
Inbrutinib IMBRUVICA® 2013 Pharmacyclics BTK CLLd, MCLe
Idelalisib ZYDELIG® 2014 Gilead PI3Kδ Haematological cancers
Cobimetinib COTELLIC® 201525 Exelixis and Genentech MEK1/2 Melanoma
Midostaurin* RYDAPT® 201726 Novartis FLT3 AMLf
Netarsudil RHOPRESSA® 201827 Aerie Pharm. Rho Kinase Glaucoma
Acalabrutinib CALQUENCE® 201728 Acerta Pharm BTK MCLe
Encorafenib BRAFTOVI® 201829 Array BioPharma B-RafV600E/K Melanoma
Larotrectinib VITRAKVI® 201830 Bayer NTRK NTRK positive solid tumors
*

Natural-product derived.

a

RCC, renal cell carcinoma.

b

RA, rheumatoid arthritis.

c

NSCLC, non-small cell lung cancer.

d

CLL, chronic lymphocytic leukemia.

e

MCL, mantle cell lymphoma.

f

AML, acute myeloid leukemia.