Common genes and corresponding FDA-approved drugs for targeted therapy
| Gene | Drug name | FDA-approved indications | Approval date |
|---|---|---|---|
| EGFR | Gefitinib | First-line, second-line, or beyond for EGFR-mutant locally advanced or metastatic non-small cell lung cancer (mNSCLC) | 2003 (US), 2004 (China) |
| Erlotinib | First-line, second-line, or beyond for EGFR-mutant mNSCLC; with gemcitabine for locally advanced, unresectable, or metastatic pancreatic cancer; first- or second-line treatment for metastatic renal cell carcinoma | 2004 (US), 2012 (China) | |
| Icotinib | First-line, second-line, or beyond for EGFR-mutant mNSCLC | 2011 (China) | |
| Afatinib | First-line treatment for EGFR-mutant mNSCLC; first- or second-line for locally advanced or mNSCLC with T790M mutations after EGFR-TKI failure; HER-2 positive metastatic breast cancer (mBC) | 2013 (US), 2014 (China) | |
| Osimertinib | First-line, second-line, or beyond for EGFR-mutant mNSCLC | 2015 (US), 2016 (China) | |
| Dacomitinib | First-line, second-line, or beyond for EGFR-mutant mNSCLC | 2018 (US), 2019 (China) | |
| Necitumumab | In combination with gemcitabine and cisplatin for first-line treatment of metastatic squamous NSCLC | 2015 (US) | |
| Neratinib | For patients with high-risk breast cancer (BC) who have completed adjuvant trastuzumab-based therapy without disease progression | 2017 (US) | |
| Panitumumab | As monotherapy or after failure of 5-FU, oxaliplatin, and irinotecan-based chemotherapy in RAS wild-type metastatic colorectal cancer (mCRC) | 2006 (US) | |
| Cetuximab | As monotherapy or combined with irinotecan for EGFR-expressing, irinotecan-refractory, RAS wild-type mCRC; combined with chemotherapy for advanced (metastatic) squamous cell carcinoma of the head and neck | 2004 (US), 2013 (China) | |
| Nimotuzumab | Combined with radiotherapy for EGFR-positive stage III/IV nasopharyngeal carcinoma | 2008 (China) | |
| HER-2 | Trastuzumab | Monotherapy for HER-2 overexpressing mBC after one or more chemotherapy regimens; combined with paclitaxel or docetaxel for HER-2 overexpressing mBC with no prior chemotherapy; adjuvant monotherapy for HER-2 overexpressing breast cancer after surgery, anthracycline-based chemotherapy, and radiotherapy | 1998 (US), 2001 (China) |
| Trastuzumab emtansine (T-DM1) | Monotherapy for HER-2 overexpressing mBC previously treated with trastuzumab and taxanes, alone or in combination | 2013 (US) | |
| Trastuzumab-DKST | Adjuvant monotherapy for HER-2 overexpressing BC post-surgery, anthracycline-based chemotherapy, and radiotherapy; monotherapy for HER-2 overexpressing mBC after one or more chemotherapy regimens; combined with paclitaxel or docetaxel for HER-2 overexpressing mBC with no prior chemotherapy | 2017 (US) | |
| Trastuzumab-PKRB | Adjuvant monotherapy for HER-2 overexpressing BC post-surgery, anthracycline-based chemotherapy, and radiotherapy; monotherapy for HER-2 overexpressing mBC after one or more chemotherapy regimens; combined with paclitaxel or docetaxel for HER-3 overexpressing mBC with no prior chemotherapy | 2019 (US) | |
| ALK | Crizotinib | First-line treatment for ALK-positive locally advanced or mNSCLC; first-line for ROS1-positive NSCLC | 2011 (US), 2017 (China) |
| Alectinib | First-line treatment for ALK-positive locally advanced or mNSCLC; second-line for ALK-positive NSCLC resistant to crizotinib | 2015 (US), 2018 (China) | |
| Ceritinib | First-line treatment for ALK-positive locally advanced or mNSCLC; second-line for ALK-positive NSCLC resistant to crizotinib | 2014 (US), 2018 (China) | |
| Brigatinib | Second-line treatment for ALK-positive NSCLC resistant to crizotinib; second-line for NSCLC resistant to osimertinib after T790M mutation failure | 2017 (US) | |
| Lorlatinib | For mNSCLC resistant to crizotinib or at least one other ALK inhibitor | 2018 (US) | |
| VEGFR | Bevacizumab | Combined with carboplatin and paclitaxel for first-line treatment of locally advanced, metastatic, or recurrent non-squamous NSCLC; combined with erlotinib for first-line treatment of EGFR-positive mNSCLC; combined with 5-FU-based chemotherapy for mCRC; combined with interferon-α for metastatic renal cell carcinoma | 2004 (US), 2017 (China) |
| Ramucirumab | Combined with docetaxel for mNSCLC resistant to platinum-based chemotherapy; combined with paclitaxel for mGC or gastroesophageal junction adenocarcinoma resistant to fluoropyrimidine or platinum; combined with FOLFIRI for mCRC after progression with bevacizumab, oxaliplatin, and 5-FU; for hepatocellular carcinoma after sorafenib with AFP ≥400 ng/mL | 2014 (US) | |
| Anlotinib | Third-line treatment for locally advanced or mNSCLC; third-line treatment for locally advanced or metastatic small-cell lung cancer (mSCLC) | 2018 (China) | |
| Recombinant Human Endostatin | Combined with NP chemotherapy for first-line or recurrent stage III/IV NSCLC | 2005 (China) | |
| Apatinib | For mGC or gastroesophageal junction adenocarcinoma after at least two prior lines of chemotherapy | 2015 (China) | |
| Sunitinib | For unresectable or metastatic pancreatic neuroendocrine tumors; unresectable renal cell carcinoma; for gastrointestinal stromal tumor (GIST) after imatinib failure or intolerance | 2006 (US), 2007 (China) | |
| Regorafenib | For mCRC progression after 5-FU, oxaliplatin, irinotecan, or EGFR/VEGF-targeted therapy (RAS wild-type); for advanced hepatocellular carcinoma after sorafenib | 2014 (US), 2012 (China) | |
| Sorafenib | For unresectable or distant metastatic hepatocellular carcinoma; unresectable renal cell carcinoma; for locally recurrent or metastatic differentiated thyroid carcinoma resistant to radioactive iodine therapy | 2005 (US), 2006 (China) | |
| Lenvatinib | First-line treatment for unresectable hepatocellular carcinoma; combined with everolimus for advanced or metastatic renal cell carcinoma; for progressive differentiated thyroid carcinoma after radioactive iodine therapy | 2015 (US), 2018 (China) | |
| Cabozantinib | Second-line treatment for hepatocellular carcinoma; first-line treatment for advanced renal cell carcinoma | 2012 (US) | |
| Pazopanib | First-line treatment for advanced renal cell carcinoma; for advanced renal cell carcinoma after cytokine therapy | 2009 (US), 2017 (China) | |
| BRAF | Dabrafenib | Combined with trametinib for BRAF V600E-mutant mNSCLC; combined with trametinib for BRAF V600E-mutant unresectable or metastatic melanoma | 2013 (US) |
| Trametinib | Combined with dabrafenib for BRAF V600E-mutant mNSCLC; combined with dabrafenib for BRAF V600E-mutant unresectable or metastatic melanoma | 2013 (US) | |
| Sorafenib | For unresectable or distant metastatic hepatocellular carcinoma; unresectable renal cell carcinoma; for locally recurrent or metastatic differentiated thyroid carcinoma resistant to radioactive iodine therapy | 2005 (US), 2006 (China) | |
| Vemurafenib | For advanced metastatic or unresectable melanoma with BRAF mutations | 2011 (US), 2017 (China) | |
| Cobimetinib | Combined with vemurafenib for BRAF V600E or V600K-mutant unresectable or metastatic melanoma | 2015 (US) | |
| Encorafenib | Combined with binimetinib for BRAF V600E-mutant unresectable or metastatic melanoma | 2018 (US) | |
| Binimetinib | Combined with encorafenib for BRAF V600E-mutant unresectable or metastatic melanoma | 2018 (US) | |
| CDK4/6 | Palbociclib | Combined with letrozole for postmenopausal women with ER+/HER-2–advanced or metastatic BC as initial endocrine therapy | 2015 (US), 2018 (China) |
| Ribociclib | Combined with letrozole for ER+/HER-2–advanced or metastatic BC in postmenopausal women | 2017 (US) | |
| Abemaciclib | Combined with fulvestrant for ER+/HER-2–advanced or metastatic BC resistant to endocrine therapy; monotherapy for ER+/HER-2–advanced or metastatic BC after endocrine therapy and prior chemotherapy | 2017 (US) | |
| KRAS | Sotorasib | For KRAS G12C-mutant locally advanced or mNSCLC after at least one prior systemic therapy | 2021 (US) |
| Adagrasib | For adult patients with KRAS G12C-mutated locally advanced or mNSCLC who have previously received at least one prior systemic therapy | 2022 (US) |