First cancer targeting tyrosine kinase inhibitor imatinib was approved to enter the market by the US Food and Drug Administration (FDA) in 2001, since then an increasing number of small-molecule targeted drugs have been developed and approved for the treatment of cancer.
By the end of 2021, worldwide 76 small-molecule targeted antitumor drugs have been approved by the US FDA and the National Medical Products Administration (NMPA) of China.
Beside Cancer, nearly 14 other disease targeting small molecule Kinase Inhibitors were also approved worldwide during the same time period, thus making total tally to 87 approved kinase Inhibitors.
Despite great progress, small-molecule targeted anti-cancer drugs still face many challenges, such as a low response rate and drug resistance. This article carefully summarizes the approved cancer kinases inhibitors.
Recently Approved Cancer Targeting Kinases Inhibitors (between 2019-2022)
| No. | Brand | Drug | Target Kinase | Marketed by | First Approved | Cancer Indication |
| 73 | LUMAKRAS™ | Sotorasib | KRAS G12C | Amgen | 2021 | On May 28, 2021, the FDA approved Sotorasib for the treatment of adult patients with KRAS G12C-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy. |
| 72 | TRUSELTIQ™ | Infigratinib | FGFR1/2/3 | QED Therapeutics / Partner Helsinn Group | 2021 | On May 28, 2021, The FDA approved TRUSELTIQ™ (infigratinib) under the accelerated approval program for the treatment of patients with previously-treated locally advanced or metastatic cholangiocarcinoma (CCA) harboring an FGFR2 fusion or rearrangement. |
| 71 | Ukoniq | Umbralisib | PI3K-delta / CK1-epsilon | TG Therapeutics | 2021 | In Feb 2021, the FDA granted accelerated approval to Umbralisib, indicated for adults with relapsed or refractory marginal zone lymphoma (MZL) who have received at least one prior anti-CD20-based regimen; and adults with R/R Follicular Lymphoma (FL) who have received at least three prior lines of systemic therapy. |
| 70 | Cosela | Trilaciclib | CDK4/CDK6 | G1 Therapeutics | 2021 | In Feb 2021, the FDA approved trilaciclib to mitigate chemotherapy-induced myelosuppression in adult patients with small cell lung cancer. Trilaciclib dramatically improves the patient chemotherapy clinical outcome (much less loss of bone marrow), treatment experience (materially less side effects especially fatigue) and, in some cancers, may extend patient lives (in cancers other than SCLC). |
| 69 | 宜诺凯® | Orelabrutinib | BTK | InnoCare Pharma (HKEX: 09969) | 2020 | On Dec. 28, 2020, Orelabrutinib received approval from the China National Medical Products Administration (NMPA) in two indications: the treatment of patients with relapsed/refractory chronic lymphocytic leukemia (CLL) /small lymphocytic lymphoma (SLL), and the treatment of patients with relapsed/refractory mantle cell lymphoma (MCL). |
| 68 | Klisyri® | Tirbanibulin | Src | Athenex, Inc. | 2020 | In Dec 2020, FDA approved, Tirbanibulin as a first-in-class Src kinase signaling inhibitor and tubulin polymerisation,approved for the treatment of actinic keratosis on the face or scalp. |
| 67 | Gavreto | Pralsetinib | RET | Blueprint Medicines | 2020 | On Sep 4, 2020, the FDA granted accelerated approval to pralsetinib for the treatment of adult patients with metastatic rearranged during transfection (RET) fusion- positive non-small cell lung cancer (NSCLC), and adult and pediatric patients 12 years of age and older with advanced or metastatic RET-mutant medullary thyroid cancer (MTC). |
| 66 | Alunbrig | Brigatinib | ALK | ARIAD Pharmaceuticals Inc. | 2020 | On May 22, 2020, the FDA approved brigatinib (, ) for adult patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) as detected by an FDA-approved test. |
| 65 | Tabrecta | Capmatinib | MET | Novartis | 2020 | On May 2020, Novartis secured accelerated approval in the US for Tabrecta, the first targeted therapy for advanced non-small cell lung cancer (NSCLC) with a specific genetic biomarker known as MET exon 14 skipping. |
| 64 | Retevmo | Selpercatinib | RET | Loxo Oncology | 2020 | In May 2020, FDA approved Selpercatinib, for the treatment of non-small cell lung cancer, medullary thyroid cancer, and other types of thyroid cancers in people whose tumors have an alteration (mutation or fusion) in a specific gene (RET or "rearranged during transfection"). |
| 63 | Tukysa | Tucatinib | HER2 | Seattle Genetics | 2020 | In April 2020, the FDA approved in combination with trastuzumab and capecitabine, for adult patients with advanced unresectable or metastatic HER2-positive breast cancer, including patients with brain metastases, who have received one or more prior anti-HER2-based regimens in the metastatic setting. |
| 62 | Pemazyre | Pemigatinib | FGFR | Incyte Corporation | 2020 | On April 2020, FDA approved pemigatinib to treat certain patients with cholangiocarcinoma, a rare form of cancer that forms in bile ducts. |
| 61 | Qinlock | Ripretinib | KIT, PDGFRa | Dicephera Pharmaceuticals | 2020 | Ripretinib is a potent pan-KIT and PDGFRα kinase inhibitor; FDA approves ripretinib for advanced gastrointestinal stromal tumor on May 15, 2020, for adult patients with advanced gastrointestinal stromal tumor (GIST) who have received prior treatment with 3 or more kinase inhibitors, including imatinib.. Ripretinib binds to the 'switch pocket' of KIT, a domain that regulates the enzyme's catalytic conformation. |
| 60 | Koselugo | Selumitinib | MEK1/2 | AstraZeneca | 2020 | Selumetinib is a medication for the treatment of children, two years of age and older, with neurofibromatosis type I (NF-1), a genetic disorder of the nervous system causing tumors to grow on nerves. |
| 59 | Tepmetko | Tepotinib | MET | Merck & Co | 2020 | Tepotinib is a c-Met inhibitor, for the treatment of adults with metastatic NSCLC, whose tumors have a mutation that leads to mesenchymal-epithelial transition (MET) exon 14 skipping. Tepotinib, received first marketing approval in Japan, in March 2020, as a "line-agnostic" drug, meaning it is approved both for treatment-naive patients and for those in whom previous attempts at treatment have failed. In Feb 2021, it was approved by US FDA and was the second therapy approved by the FDA to treat non-small cell lung cancer with these particular mutations, after capmatinib. |
| 48 | Ameile | Almonertinib*** | EGFR T79M+ | Hansoh Pharmaceutical Group Company Limited | 2020 | In Mar 2020, The Chinese National Medical Products Administration has approved almonertinib (Ameile; HS-10296) for the treatment of patients with EGFR T790M mutation–positive non–small cell lung cancer who have progressed on or after other EGFR TKI therapy. |
| 57 | Ayvakit | Avapritinib | mutant PDGFR | Blueprint Medicines | 2020 | On January 2020 FDA approved avapritinib to treat adults with unresectable or metastatic gastrointestinal stromal tumor (GIST), harboring a platelet-derived growth factor receptor alpha (PDGFRA) exon 18 mutation, including D842V mutations. |
| 56 | Brukinsa | Zanubrutinib | BTK | BeiGene | 2019 | Zanubrutinib is a medication for the treatment of adults with mantle cell lymphoma (MCL) who have received at least one prior therapy. It was approved for medical use in the United States in Nov 2019. |
| 55 | Inrebic | Fedratinib | JAK2 | Sanofi | 2019 | In Aug 2019, FDA approved fedratinib to treat adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis. |
| 54 | Rozlytrek | Entrectinib | TRKA/B/C / ROS1 / ALK | Roche | 2019 | In Aug 2019, FDA approved entrectinib to treat ROS1-positive non-small cell lung cancer and NTRK fusion-positive solid tumors. Later it was approved in Australia in May 2020, and in the European Union in July 2020. |
| 53 | Turalio | Pexidartinib | CSF1R / c- KIT / FLT3 | Daiichi Sankyo | 2019 | In Aug 2019, FDA approved pexidartinib to treat adult patients with symptomatic tenosynovial giant cell tumor. |
| 52 | Piqray | Apelisib | PI3Ka | Novartis | 2019 | Alpelisib is indicated in combination with fulvestrant for the treatment of postmenopausal women, and men, with hormone receptor (HR)‑positive, human epidermal growth factor receptor 2 (HER2)‑negative, locally advanced or metastatic breast cancer with a PIK3CA mutation after disease progression following endocrine therapy as monotherapy. |
Cancer Targeting Small Molecule Kinases Inhibitors Approved (between 2015-2018)
| No. | Brand | Drug | Target Kinase | Marketed by | First Approved | Cancer Indication |
| 51 | Xospata | Gilteritinib | FLT3 / AXL | Astellas Pharma | 2018 | In Nov 2018, the FDA approved Gilteritinib for the treatment of adult patients with FLT3 mutation–positive relapsed or refractory acute myeloid leukemia (AML). |
| 50 | Vitrakvi | Larotrectinib | TRKA/B/C | Bayer | 2018 | In Nov 2018, the FDA approved larotrectinib for the treatment of Solid tumors with NTRK fusion. |
| 49 | Lorviqua | Lorlatinib | ALK/ROS1 | Novartis | 2018 | In Nov 2018, the FDA approved lorlatinib to treat patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer. |
| 48 | Copictra | Duvelisib | PI3Kγ/δ | Verastem | 2018 | In Oct 2018, the FDA approved Duvelisib for adult patients with relapsed or refractory chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) nd follicular lymphoma after at least two prior therapies. |
| 47 | Vizimpro | Dacomitinib | EGFR | Pfizer | 2018 | In Oct 2018, the FDA approved Dacomitinib for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) with epidermal growth factor receptor (EGFR) exon 19 deletion or exon 21 L858R substitution mutations as detected by an FDA-approved test. |
| 46 | Elunate | Fruquintinib*** | VEGFR-1/2/3 | Hutchison China MediTech / Lilly | 2018 | In Sep 2018, Fruquintinib received its first global approval, in China, for use in the treatment of metastatic colorectal cancer (CRC) in patients who have failed at least two prior systemic anti-neoplastic therapies. Fruquintinib is an orally available, potent and highly selective small molecule inhibitor of VEGFR-1, -2 and -3 that was discovered and developed by Hutchison MediPharma for the treatment of solid tumours. |
| 45 | Focus V | Anlotinib*** | VEGFR-2/3 / PDGFR-β / FGFRs | Chia Tai Tianqing | 2018 | Anlotinib is approved in China for the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) who have undergone progression or recurrence after ≥ 2 lines of systemic chemotherapy. |
| 44 | Irene | Pyrotinib*** | ErbB | Jiangsu Hengrui Medicine | 2018 | Pyrotinib is an irreversible dual pan-ErbB receptor tyrosine kinase inhibitor approved in China for use in combination with capecitabine for the treatment of HER2-positive, advanced or metastatic breast cancer in patients previously treated with anthracycline or taxane chemotherapy. |
| 43 | Braftovi | Encorafenib | RAF[V600E] | Novartis / Array Pharma | 2018 | In June 2018, the FDA approved encorafenib and binimetinib in combination patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. |
| 42 | Mektovi | Binimetinib | MEK1/2 | Novartis / Array Pharma | 2018 | In June 2018, the FDA approved encorafenib and binimetinib in combination patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation, as detected by an FDA-approved test. |
| 41 | Verzenio | Abernaciclib | CDK4/CDK6 | Eli Lilly | 2017 | On Sep 2017, the FDA approved abemaciclib in combination with fulvestrant or as monotherapy for women with HR-positive, HER2-negative advanced or metastatic breast cancer with disease progression following endocrine therapy. |
| 40 | Fotivda | Tivozanib | PDGFR-α / VEGFR-1/2/3 / FGFR-1/2/3/4 / c-Kit / RET | AVEO Oncology / EUSA Pharma | 2017 | In Aug 2017, the European Commission approved tivozanib as a first line treatment of adult patients with advanced renal cell carcinoma who are VEGFR and mTOR pathway inhibitor-naïve following disease progression after one prior treatment with cytokine therapy, in the European Union plus Norway and Iceland. In March 2021, The FDA granted approval to tivozanib for the treatment of adult patients with R/R RCC following 2 or more prior lines of therapy. |
| 39 | Kisqali | Ribociclib | CDK4/CDK6 | Novartis | 2017 | human epidermal growth factor receptor 2 (HER2) negative hormone-related breast cancer. |
| 38 | Nerlynx | Neratinib | HER2 | Puma Biotechnology | 2017 | For use as an extended adjuvant treatment in adult patients with early stage HER2-overexpressed/amplified breast cancer, to follow adjuvant trastuzumab-based therapy |
| 37 | Aliqopa | Copanlisib | TOR/PI-3Kd | Bayer | 2017 | Indicated for the treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies. |
| 36 | Calquence | Acalabrutinib | BTK | AstraZeneca | 2017 | Acalabrutinib is currently indicated for the treatment of adult patients with Mantle Cell Lymphoma (MCL) who have received at least one prior therapy. |
| 35 | Akunbrig | Brigatinib | ALK / ROS / IGF1R / EGFR / FLT3 | Ariad Pharmaceuticals | 2017 | Brigatinib is indicated for the treatment of patients with ALK+ NSCLC with intolerance to Crizotinib. |
| 34 | Rydapt | Midostaurin | FLT3 / c-Kit | Novartis | 2017 | Acute Myeloid Leukemia |
| 33 | Olita | Olmutinib** | mutant EGFR | Hanmi Pharmaceutical / Boehringer Ingelheim | 2016 | Olmutinib is an oral third-generation EGFR mutant-specific kinase inhibitor that was granted breakthrough therapy designation by US FDA in 2015 and received the first approval for the treatment of patients with EGFR T790M mutation-positive NSCLC in South Korea in 2016. |
| 32 | Alecensa | Alectinib | ALK | Roche / Chugai | 2015 | Treatment of patients with anaplastic lymphoma kinase (ALK)-positive, metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. |
| 31 | Ibrance | Palbociclib | CDK4/CDK6 | Pfizer | 2015 | Palbociclib is indicated in combination with letrozole for the treatment of postmenopausal women with estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative advanced breast cancer as initial endocrine-based therapy for their metastatic disease. |
| 30 | Lenvima | Lenvatinib | PDGFR-α / VEGFR-1/2/3 / FGFR-1/2/3/4 / c-Kit / RET | Eisai | 2015 | Lenvatinib is indicated for the treatment of patients with locally recurrent or metastatic, progressive, radioactive iodine-refractory differentiated thyroid cancer. DTC (2015) Thyroid cancer (2015) RCC (2016) HCC (2018) Endometrial carcinoma (2019) |
| 29 | Cotellic | Cobimetinib | MEK1/2 | Roche / Genentech / Exelixis | 2015 | For the treatment of patients with unresectable or metastatic melanoma with a BRAF V600E or V600K mutation. Cobimetinib is used in combination with vemurafenib, a BRAF inhibitor. |
| 28 | Tagrisso | Osimertinib | mutant EGFR | AstraZeneca | 2015 | Osimertinib is indicated for the treatment of patients with metastatic epidermal growth factor receptor (EGFR) T790M mutation-positive non-small cell lung cancer (NSCLC), as detected by an FDA- approved test, who have progressed on or after EGFR-TKI therapy. |
Cancer Targeting Small Molecule Kinases Inhibitors Approved (between 2001-2014)
| No. | Brand | Drug | Target Kinase | Marketed by | First Approved | Cancer Indication |
| 27 | Zykadia | Ceritinib | ALK / ROS | Novartis | 2014 | Treatment of patients with anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC) who have progressed on or are intolerant to crizotinib. |
| 26 | Zydelig | Idelalisib | PI3Kδ | Gilead | 2014 | Approved for the treatment of chronic lymphocytic leukemia (CLL) as a second-line agent in combination with rituximab and for relapsed follicular B-cell non-Hodgkin lymphoma (FL) and relapsed small lymphocytic lymphoma (SLL) in patients who have received at least two prior systemic therapies. |
| 25 | Aitan | Apatinib** | VEGFR-2 / Src / c-Kit | Hengrui Medicine | 2014 | Apatinib inhibits the activities of VEGFR-2, c-Src, and c-Kit simultaneously and was approved by the NMPA of China for the treatment of advanced gastric cancer in Oct 2014. |
| 24 | Imbruvica | Ibrutinib | BTK | AbbVie (Pharmacyclics) / Johnson & Johnson | 2013 | Ibrutinib was approved by the FDA for the treatment of Mantle Cell Lymphoma, and later in February 2014 for the treatment of Chronic Lymphocytic Leukemia. Later approved for Waldenström's macroglobulinemia (2015), Small lymphocytic lymphoma (SLL) (2016) with or without 17p deletion and mantle cell lymphoma (2017) |
| 23 | Tafinlar | Dabrafenib | BRAF[V600E] / CRAF | Novartis / GlaxoSmithKline | 2013 | In patients with unresectable or Metastatic Melanoma with BRAF V600E mutation as detected by an FDA-approved test. In April 2017, the EU approved the combination of Dabrafenib with Trametinib for BRAF V600+ Advanced Non small-cell lung cancer (2017) and for BRAF V600–Mutant Anaplastic Thyroid Cancer (2018). |
| 22 | Mekinist | Trametinib | MEK1 / MEK2 | Novartis / GlaxoSmithKline | 2013 | Trametinib is indicated for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations, as detected by an FDA-approved test. It was also approved in combination with Dabrafenib for NSCLC (2017) and ATC (2018). |
| 21 | Giotrif | Afatinib | EGFR | Boehringer Ingelheim | 2013 | First-line treatment of patient with metastatic non-small cell lung cancer (NSCLC) whose tumours have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test. |
| 20 | Cabometyx | Cabozantinib | VEGFR-1/2/3 / TYRO3 / ROS / TIE2 / c-Met / HGFR / c-Kit / TRK2 / RET | Exelixis | 2012 | For the treatment of Metastatic Medullary Thyroid Cancer (2012); in patients with advanced Renal Cell Carcinoma (2016) who have received prior anti-angiogenic therapy and Hepatocellular Carcinoma (2019). |
| 19 | Iclusig | Ponatinib | Bcr-Abl / PDGFR-α / VEGFR-2 / FGFR-1 / Src / FLT3 / c-Kit | Ariad Pharmaceuticals / Takeda | 2012 | Treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive Acute Lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy. |
| 18 | Supect | Radotinib** | Bcr-Abl | Ilyang Pharmaceutical / Daewoong Pharmaceutical | 2012 | Radotinib is a novel and selective second-generation BCR-ABL1 TKI, which is currently approved in Korea for the treatment of patients with CML. |
| 17 | Inlyta | Axitinib | VEGFR-1/2/3 / PDGFR | Pfizer | 2012 | Renal Cell Carcinoma |
| 16 | Bosulif | Bosutinib | BCR Abl1 / Src / CDK2 / LYN | Pfizer | 2012 | Treatment of chronic, accelerated, or blast phase Philadelphia chromosome-positive (Ph+) chronic myelogenous leukemia (CML) with resistance or intolerance to prior therapy in adult patients. |
| 15 | Stiverga | Regorafenib | VEGFR-1/2/3 / PDGFR-α/β / FGFR-1/2 / RAF / RET / c- Kit | Bayer | 2012 | Treatment of patients with metastatic colorectal cancer (CRC) (2012) who have been previously treated with fluoropyrimidine-, oxaliplatin- and irinotecan-based chemotherapy, an anti-VEGF therapy, and, if KRAS wild type, an anti-EGFR therapy. Regorafenib is also indicated for the treatment of patients with locally advanced, unresectable or metastatic gastrointestinal stromal tumor (GIST) (2013) who have been previously treated with imatinib mesylate and sunitinib malate and Hepatocellular Carcinoma (2017). |
| 14 | Xalkori | Crizotinib | ALK / ROS1 | Pfizer | 2011 | Crizotinib is used for the treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) that is anaplastic-lymphoma kinase (ALK)-positive as detected by a FDA-approved test. |
| 13 | Caprelsa | Vandetanib | EGFR / VEGFR / RET / BRK / TIE2 / EPH | Genzyme | 2011 | Vandetanib is indicated for the treatment of symptomatic or progressive medullary thyroid cancer in patients with unresectable locally advanced or metastatic disease. |
| 12 | Jakavi | Ruxolitinib | JAK 1,2 | Incyte Corporation / Novartis | 2011 | Treatment of intermediate or high-risk myelofibrosis. Myeolofibrosis is the proliferation of abnormal bone marrow stem cells which cause fibrosis (the excessive formation of connective tissue). |
| 11 | Zelboraf | Vemurafenib | BRAF[V600E] | Roche | 2011 | Approved for the treatment of metastatic melanoma with a mutation on BRAF in the valine located in the exon 15 at codon 600, this mutation is denominated as V600E. |
| 10 | Conmana | Icotinib*** | EGFR | Zhejiang Beta Pharma | 2011 | In patients with advanced non-small-cell lung cancer (NSCLC) who failed previous chemotherapy. |
| 9 | Votrient | Pazopanib | PDGFR-β / VEGFR-1/2/3 / FGFR-1/3 / c-Kit / Itk / Lck / c-GSK | Novartis | 2009 | Treatment of advanced Renal cell cancer (2009) and advanced soft tissue sarcoma (2012) (in patients previously treated with chemotherapy) |
| 8 | Tyverb | Lapatinib | EGFR / Her2 | Novartis | 2007 | Indicated in combination with capecitabine for the treatment of patients with advanced breast cancer whose tumors overexpress HER2 protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma. |
| 7 | Tasigna | Nilotinib | Bcr-Abl / DDR1/2 | Novartis | 2007 | For the potential treatment of various leukemias, including chronic myeloid leukemia (CML). |
| 6 | Sutent | Sunitinib | PDGFR-α/β / VEGFR-1/2/3 / CSF1R / c-Kit / RET / FLT3 | Pfizer | 2006 | For the treatment of advanced renal cell carcinoma (2006) ; Gastrointestinal stromal tumor (2006) after disease progression on or intolerance to imatinib mesylate and Pancreas neuroendocrine tumor (2011). |
| 5 | Sprycel | Dasatinib | Bcr-Abl / Src / c-Kit / LCK / PDGFR-β | Bristol Myers Squibb | 2006 | For the treatment of adults with chronic, accelerated, or myeloid or lymphoid blast phase chronic myeloid leukemia (CML) with resistance or intolerance to prior therapy. Also indicated for the treatment of adults with Philadelphia chromosome-positive acute lymphoblastic leukemia (ALL) with resistance or intolerance to prior therapy. |
| 4 | Nexavar | Sorafenib | c-Kit / FLT3 / RET / PTC / VEGFR-1/2/3 / PDGFR-β | Bayer | 2005 | Sorafenib is indicated for the treatment of advanced Renal Cell Carcinoma (2005); Unresectable Hepatocellular Carcinoma (2007), DTC (2013) and Thyroid Cancer (2014) |
| 3 | Tarceva | Erlotinib | EGFR | Osi Pharmaceuticals | 2004 | For the treatment of patients with locally advanced or metastatic NSCLC after failure of at least one prior chemotherapy regimen. Also for use, in combination with gemcitabine, as the first-line treatment of patients with locally advanced, unresectable or metastatic pancreatic cancer (2005). |
| 2 | Iressa | Gefitinib | EGFR | AstraZeneca | 2002 | For the continued treatment of patients with locally advanced or metastatic NSCLC, after failure of either platinum-based or docetaxel chemotherapies. |
| 1 | Gleevec | Imatinib | Abl / c-KIT / CSF1R / PDGFR | Novartis | 2001 | Ph+ Chronic Myeloid Leukemia (CML), Ph+ Acute Lymphoblastic Leukaemia, Malignant gastrointestinal stromal tumors (GIST) |
