Table 1.
General information on anti-cancer TKI
| 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Expired and withdrawn |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Withdrawn |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1-3, PDGFR-A, PDGFR-B; KIT, FLT3 | Renal cell carcinoma, GIST, pNET | 19th July 2006 | Initially, then full approval | Withdrawn |
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].