Table 3.
Comparison of MTD to package insert dose of small molecule inhibitors used to treat solid malignancies.
| Drug | MTD1 | Package Insert Dose / Dose under development | Dosed below MTD |
|---|---|---|---|
| afatinib | 50mg daily | 40mg daily | X |
| alectinib | 900mg bid | 600mg bid | X |
| axitinib | 5mg bid | 5mg bid | |
| brigatinib2 | 300mg daily | 180mg daily | X |
| cabozantinib | 175mg daily | 140mg daily | X |
| ceritinib | 750mg daily | 750mg daily | |
| cobimetinib | 60mg daily3 | 60mg daily3 | |
| crizotinib | 250mg bid | 250mg bid | |
| dabrafenib | 300mg bid | 150mg bid | X |
| erlotinib | 150mg daily | 150mg daily | |
| everolimus | 10mg daily4 | 10mg daily | |
| gefitinib | 600mg daily | 250mg daily | X |
| imatinib | 400mg bid | 400-600mg daily | X |
| lapatinib | 1500mg daily4,5 | 1500mg daily5 | |
| lenvatinib | 25mg daily | 24mg daily | X |
| olaparib | 400mg bid | 400mg bid | |
| olmutinib2 | 800mg daily | 800mg daily | |
| osimertinib | 240mg daily4 | 80mg daily | X |
| palbociclib | 125mg daily3 | 125mg daily3 | |
| pazopanib | 2000mg daily | 800mg daily | X |
| regorafenib | 160mg daily3 | 160mg daily3 | |
| rociletinib2 | 1000mg bid4 | 500mg bid | X |
| sonidegib | 800mg daily | 200mg daily | X |
| sorafenib | 400mg bid | 400mg bid | |
| sunitinib | 50mg daily6 | 50mg daily6 | |
| temsirolimus | 250mg weekly4 | 25mg weekly | X |
| trametinib | 3mg daily | 2mg daily | X |
| vandetanib | 300mg daily | 300mg daily | |
| vemurafenib | 960mg bid | 960mg bid | |
| vismodegib | 540mg daily4 | 150mg daily | X |
1
References for determination of MTD provided in Supplementary Table 2
2
Given breakthrough status by FDA for the treatment of lung cancer
3
Administered in a 3 weeks on, 1 week off cycle
4
Maximum tested dose rather than maximum tolerated dose
5
MTD tested and FDA-approved in combination with letrozole for HER2 positive metastatic breast cancer
6
Admininsterd in a 4 weeks on, 2 weeks off cycle