Table 5. Examples of Healthy Volunteer (HV) studies testing MTA.
| Type of HV study | MTA | Mechanism of action | Endpoints of the study | Healthy subject dose | Status | ClinicalTrials.gov identifier |
|---|---|---|---|---|---|---|
| Drug-drug |
PF-00299804 (dacomitinib) |
Pan-HER inhibitor | Pharmacokinetic. To asses interactions between paroxetine and dacomitinib. |
Single doses 45 mg dacomitinib with or without 30 mg paroxetine | Ph1 completed | NCT01318031 |
| Food-drug |
AG-013736 (axitinib) |
VEGFR, PDGFR, c-KIT inhibitor |
Pharmacokinetic. To assess the food effect on drug levels. |
Single doses axitinib in different fasting conditions | Ph1 completed | NCT00918632 |
| Cardiovascular Safety |
SOM230 (pasireotide) |
Somatostatin analogue | Safety. To assess cardiac repolarization. |
Therapeutic pasireotide dose 600ug vs MTD vs placebo vs moxifloxacin | Ph1 completed | NCT01128192 |
| Bioavailability | SR13668 | AKT inhibitor | Pharmacokinetic. To determine the best bioavailable formulation. |
Single doses of SR13668 testing different formulations | Ph1 completed | NCT00896207 |
| Bioequivalence | PF-05280014 | Anti-EGFR2 inhibitor | Pharmacokinetic. To assess bioequivalence between PF-05280014 and approved TTZ. |
PF-05280014 vs TTZ-EU vs TTZ-US | Ph1 completed | NCT01603264 |
| Ph1 FIH |
ARRY-142866 (selumetinib) |
MEK1/2 inhibitor | Pharmacokinetic, safety and tolerability. | Single doses of 25 mg selumetinib, and with or without itraconazol or fluconazol | Ph1 completed | NCT02093728 |
Abbreviations: MTA (Molecularly Targeted Agents); HER (Human Epidermal growth factor Receptor); VEGFR (Vascular Endothelial Growth Factor Receptor); PDGFR (Platelet Derived Growth Factor Receptor); MTD (Maximum Tolerated Dose); EGFR2 (Epidermal Growth Factor Receptor 2); TTZ (TrasTuZumab); vs (versus); EU (European Union); US (United States).