Table 4.
Ongoing clinical trials involving MKIs with RET inhibition activity in MTC.
| Drug | Combination | Drug Targets | Population | Phase | N | Primary Endpoint | Status | Results |
|---|---|---|---|---|---|---|---|---|
| Selpercatinib (LOXO-292) NCT03157128 |
N/A | RET | Advanced solid tumors | I/II | 970 | MTD, RP2D, ORR | Recruiting | 56% [104] |
| Selpercatinib (LOXO-292) NCT04211337 |
Cabozantinib Vandetanib |
RET | RET-m MTC | III | 400 | TFFS | Recruiting | Not available |
| Pralsetinib (BLU-667) NCT03037385 |
N/A | RET | Advanced solid tumors | I/II | 527 | MTD, ORR | Recruiting | 89% [107] |
| Anlotinib NCT02586350 |
N/A | VEGFR, FGFR, PDGFR, c-kit, RET | MTC | IIB | 91 | PFS | Completed | 20.67 months [108] |
| Surufatinib NCT02614495 |
N/A | VEGFR, FGFR, RET | RAI-R DTC, MTC |
II | 66 | ORR | Completed | PR 17% [109] |
| Nintedanib NCT01788982 |
N/A | VEGFR, FGFR, PDGFR, RET | DTC, MTC | II | 143 | PFS | Active, not recruiting | Not available |
| Regorafenib NCT02657551 |
N/A | VEGFR, PDGFR, c-kit, RET | MTC | II | 33 | PFS | Recruiting | Not available |
| BOS172738 NCT03780517 |
N/A | VEGFR, RET | RET-gene altered tumors | I | 144 | TEAE, MTD, RP2D | Recruiting | Not available |
| TPX-0046 NCT04161391 |
N/A | SRC, RET | RET-gene altered tumors | I/II | 362 | DLTs, MTD, ORR | Recruiting | Not available |
RAI-R DTC: radioiodine-refractory differentiated thyroid cancer, MTC: medullary thyroid cancer, MTD: maximum tolerated dose, RP2D: recommended phase 2 dose, ORR: objective response rate, PFS: progression free survival, TFFS: treatment failure free survival, TEAE: treatment emergent adverse event, DLTs: dose-limiting toxicities, N/A: not/applicable.