Table 1.
Agents targeting epidermal growth factor receptors and downstream molecules under clinical investigation for the treatment of drug-resistant and metastatic colorectal cancer
|
Agent
|
Targeted molecule
|
Condition
|
Study phase
|
Clinical trial identifier
|
| Erlotinib | EGFR | First-line treatment for mCRC | Phase III | NCT01229813 |
| Futuximab/Modotuximab (Sym-004) | EGFR | mCRC | Phase II | NCT02083653 |
| Gefitinib | EGFR | Refractory CRC | Phase I/II | NCT00242788 |
| Afatinib | EGFR | Refractory mCRC | Phase II | NCT01919879 |
| Advanced CRC | Phase II | NCT00801294 | ||
| mCRC | Phase II | NCT01152437 | ||
| Dabrafenib (GSK2118436) | BRAF | mCRC | Phase II | NCT03668431 |
| mCRC | Phase II | NCT03428126 | ||
| BMS-908662 | BRAF | K-RAS/BRAF-mutated CRC | Phase I/II | NCT01086267 |
| Encorafenib | Wild-type and BRAF V600E | Previously untreated BRAF-mutant mCRC | Phase II | NCT03693170 |
| Vemurafenib | Mutated BRAF V600E | BRAF V600E mutated advanced CRC | Phase II | NCT03727763 |
| PX-866 | PI3K | mCRC | Phase I/II | NCT01252628 |
| Gedatolisib | PI3K/mTOR | KRAS/NRAS-wild-type mCRC | Phase II | NCT01925274 |
| mCRC | Phase I/II | NCT01937715 | ||
| Temsirolimus CCI-770 | mTOR | KRAS-mutated mCRC | Phase II | NCT00827684 |
| Cetuximab-refractory CRC | Phase I | NCT00593060 | ||
| Everolimus (RAD001) | mTOR | mCRC | Phase II | NCT01387880 |
| mCRC | Phase I/II | NCT01058655 | ||
| Advanced mCRC | Phase I/II | NCT01139138 | ||
| Refractory mCRC | Phase I | NCT01154335 | ||
| MK-2206 | AKT | Advanced CRC | Phase II | NCT01333475 |
| Napabucasin (BBI608) | STAT3 | Previously treated mCRC | Phase III | NCT03522649 |
| Cobimetinib | MAPK | mCRC | Phase III | NCT02788279 |
| Selumetinib | MEK | mCRC | Phase II | NCT00514761 |
| Binimetinib | MEK | Previously untreated BRAF-mutant mCRC | Phase II | NCT03693170 |
| Neratinib | EGFR/HER2/4 | KRAS/NRAS/BRAF/PIK3CA-wild-type mCRC | Phase II | NCT03457896 |
| Sapitinib (AZD-8931) | EGFR/HER2/3 | mCRC | Phase II | NCT01862003 |
| Duligotuzumab (MEHD7945A) | EGFR/HER3 | KRAS-mutated mCRC | Phase II | NCT01652482 |
| Trastuzumab | HER2 | First-line HER2-positive mCRC | Phase III | NCT05253651 |
| Tucatinib | HER2 | First-line HER2-positive mCRC | Phase III | NCT05253651 |
| Disitamab Vedotin | HER2 | HER2-positive advanced CRC | Phase II | NCT05493683 |
| HER2-expressing mCRC | Phase II | NCT05333809 | ||
| Trastuzumab-emtansine | HER2 | HER2-positive mCRC progressing after trastuzumab and lapatinib | Phase II | NCT03418558 |
EGFR: Epidermal growth factor receptor; mCRC: Metastatic colorectal cancer; PI3K: Phosphoinositide 3-kinases; mTOR: Mammalian target of rapamycin; STAT3: Signal transducer and activator of transcription 3; AKT: Protein kinase B; MAPK: Mitogen-activated protein kinases; MEK: Mitogen-activated extracellular signal-regulated kinase; HER2: Human epidermal growth factor receptor 2.