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Table 1 General information on anti-cancer TKI

From: Clinical pharmacology of tyrosine kinase inhibitors becoming generic drugs: the regulatory perspective

Tyrosine kinase inhibitor (INN)

Branded name

Market Authorization Holder (MAH)

Target tyrosine kinases

Indication(s)

European birth date

CMA

Orphan designation

Bosutinib

Bosulif®

Pfizer

BCR-ABL,SRC

Patients with CML for which Imatinib, Nilotinib, and Dasatinib are not appropriate

27th March 2013

Yes

CML

Dasatinib

Sprycel®

Bristol-Myers Squibb

BCR-ABL

CML

23th December 2005

No

CML, ALL

Erlotinib

Tarceva®

Hoffman-La Roche

EGFR

NSCLC, pancreatic cancer

19th September 2005

No

No

Gefitinib

Iressa®

Astra Zeneca

EGFR

NSCLC in carriers of activating EGFR-mutations

24th June 2010

No

No

Imatinib

Glivec®

Novartis

BCR-ABL, KIT, PDGFR-A, PDGFR-B

CML, GIST, BCR-ABL- positive ALL, dermatofibrosarcoma protuberans, myeloproliferative neoplasms, hypereosinophilic syndromes

7th of November 2001

No

Expired and withdrawn

Lapatinib

Tyverb®

Glaxo Smith Kline

ERBB2 (HER-2)

HER-2 positive breast cancer

10th June 2008

Yes

No

Nilotinib1

Tasigna®

Novartis

BCR-ABL, KIT,PDGFR-A, PDGFR-B

CML

19th November 2007

No

CML

Pazopanib

Votrient®

Glaxo Smith Kline

VEGFR, PDGFR, KIT

Renal cell carcinoma, STS

14th June 2010

No

Withdrawn

Ponatinib2

Iclusig®

Ariad

BCR-ABL

Patients with CML for which Imatinib, Nilotinib, and Dasatinib are not appropriate (or patients carrying a T315I single-point-mutation)

1st July 2013

 

CML, ALL

Sorafenib

Nexavar®

Bayer

VEGFR-2,VEGFR-3

Renal cell carcinoma, hepatocellular carcinoma

19th July 2006

No

Renal cell carcinoma, Hepatocellular carcinoma

Sunitinib

Sutent®

Pfizer

VEGFR 1-3, PDGFR-A, PDGFR-B; KIT, FLT3

Renal cell carcinoma, GIST, pNET

19th July 2006

Initially, then full approval

Withdrawn

  1. ALL, acute lymphatic leukemia; CML, chronic myeloid leukemia ; CMA, Conditional Marketing Authorization (none of the above mentioned is currently authorized under exceptional circumstances, according to European Medicines Agency (EMA) website accessed in Sept 2013 [15]); GIST, gastrointestinal stromal tumor; MA, Marketing Authorization; MAH, Marketing Authorization Holder; NSCLC, non-small cell lung cancer; pNET, pancreatic neuroendocrine tumors; STS, soft tissue sarcoma; 1Nilotinib is similar to Imatinib according to the orphan regulation; 2US-Food and Drug Administration (FDA) asked the manufacturer of Ponatinib to suspend marketing due to the risk of life-threatening blood clots and severe narrowing of blood vessels; source of information: European Public Assessment Reports (EPARs) of the above mentioned TKI [15].