Table 3.
Molecular and clinical characteristics of the target-based drugs used in CCA.
| Target | Drug | Molecular Weight (Da) | Type of Inhibition | IC50 * | Most Common Clinical Toxicities (All Grades) |
|---|---|---|---|---|---|
| FGFR | Pemigatinib | 487.50 | Reversible | 0.5 nM/L * | Diarrhea, fatigue, alopecia, and eye tox |
| Infigratinib | 560.48 | Reversible | 1.4 nM/L * | Eye tox, stomatitis, and fatigue | |
| Derazantinib | 468.57 | Reversible | 1.8 nM/L * | Eye tox, stomatitis, and fatigue | |
| Futibatinib | 418.45 | Irreversible | 1.4 nM/L * | Nail tox, fatigue, and musculoskeletal tox | |
| IDH1 | Ivosidenib | 582.96 | Reversible | 70.0 nM/L | Diarrhea, neutropenia, leukocytosis, and fatigue |
| BRAF | Vemurafenib | 482.92 | Reversible | 31 nM/L | Alopecia, arthralgia, fatigue, and eye tox |
| Dabrafenib | 519.56 | Reversible | 0.7 nM/L | Fever, neutropenia, and fatigue | |
| NTRK | Larotrectinib | 526.51 | Reversible | 11 nM/L ** | Anemia, fatigue, and nausea |
| Entrectinib | 560.63 | Reversible | 1 nM/L ** | Dysgeusia, fatigue, and diarrhea | |
| HER2 | Trastuzumab | 145,531.5 | Reversible | 1 mg/mL | Fever, nausea, allergy, and diarrhea |
Da: Daltons; IC50: inhibitory concentration by 50%; Tox: toxicity. * All IC50, except for HER row, refer to cell-free assays (kinase activity); * IC50 on FGFR2 activity; ** IC50 on TRKA activity.