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Table 3 Selected published trials of oncology drugs in healthy volunteers sorted by study objective

From: Reviewing the role of healthy volunteer studies in drug development

NCT number, PMID number Treatment Target/MOA Study population/study design Study objective/study endpoints Enrolled (N)
Mass balance
 NCT01674322, 25488930 [47] [14C]-Ibrutinib Bruton tyrosine kinase Single center, open-label, single-dose study in healthy males PK of total radioactivity, parent drug and metabolites (plasma, urine, feces) based on CYP2D6 genotype 6 (2 CYP2D6 poor metabolizer subjects)
 NCT01711762, 26451002 [46] [14C]-Cobimetinib MEK inhibitor Single center, open-label, nonrandomized study in healthy males PK of total radioactivity, parent drug and metabolites (plasma, urine, feces) 6
Bioequivalence
 N/A, 26272586 [52] Ceritinib ALK inhibitor Two randomized, open-label, 2-period, crossover studies in healthy subjects Changes in bioavailability with low- or high-fat meal, or light snack compared to fasting conditions 40 (28, 12)
 N/A, 25643050 [53] Erlotinib EGFR inhibitor Two single center, open-label, crossover studies (two and three sequence) in healthy subjects Changes in bioavailability when coadministered with ranitidine or omeprazole 48 (24 each)
 N/A, 28776077 [57] Abiraterone Acetate CYP17 inhibitor Single center, open-label, fixed treatment sequence, 3-period, single-dose, crossover study in healthy males Changes in bioavailability with novel formulation under both fasted and fed conditions compared with historical controls 11
Biosimilarity
 NCT01603264, 25041377 [80] Trastuzumab (PF-05280014, EU-, or US-approved trastuzumab) HER2 inhibitor Single center, double-blind, parallel group, single-dose, 3-arm, active comparator trial in healthy subjects Establish 3-way clinical PK similarity of PF-05280014 to both EU- and US-trastuzumab formulations, and of EU- to US-trastuzumab 101
 NCT01608087, 28651442 [59] Bevacizumab, (BI 695502, US-, or EU-approved bevacizumab) VEGF inhibitor Two center, randomized, single-blind, single-dose, two-stage, 3 parallel-arm, active-comparator trial in healthy subjects Establish 3-way clinical PK similarity to enable use of just one reference product for a Phase III biosimilarity trial 91
Drug–drug interaction
 NCT01147055, NCT01149785, 26381275 [81] Crizotinib ALK inhibitor Two single center, open-label, 2-period, 2-treatment, 1-sequence, single-dose, crossover studies in healthy subjects Estimate the effects of multiple doses of ketoconazole and rifampin on single-dose PK 30 (15 each)
 N/A, 20702754 [66] Nilotinib BCR/ABL inhibitor Two single center, open-label, 2-period, 1 sequence, single-dose crossover studies in healthy subjects Estimate the effects of multiple doses of ketoconazole and rifampin on single-dose PK 15 (rifampin) 26 (ketoconazole)
Organ impairment
 NCT01298063, 24906422 [68] Afatinib EGFR inhibitor Single center, open-label, single-dose study comparing mild (n = 8) and moderate hepatic impairment (n = 8) to matched healthy controls (n = 16) Compare relative drug exposure between subjects with hepatic impairment and matched healthy controls, as measured by AUC0−∞ and Cmax 32
 NCT02096718, 27436099 [69] Single center, open-label, single-dose study comparing moderate (n = 8) and severe renal impairment (n = 8) to matched healthy controls (n = 14) Compare relative drug exposure between subjects with renal impairment and matched healthy controls, as measured by AUClast and Cmax 30
Pharmacokinetic/pharmacodynamic relationships
 N/A, 28660498 [70] Degarelix GnRH antagonist Single center, double-blind (open-label for moxifloxacin) randomized, crossover study in healthy males Compare the effect of single-dose degarelix, placebo, and moxifloxacin on the QT interval 80
 NCT00406406, 22884766 [64] Bosutinib Src/Abl inhibitor Single-center, randomized, double-blind, placebo-controlled, single-ascending dose, sequential-group study in healthy subjects Assess the safety, tolerability, and PK with ascending doses to support further clinical pharmacology assessment 48
 N/A, 20376000 [73] Sunitinib PDGFR/VEGFR/KIT/FLT3/CSF1R/RET inhibitor Single center, open-label, multiple dose study in healthy subjects To develop a PD/PK model to investigate the concentration-effect relationship between drug and biomarkers (blood pressure, VEGF-A, VEGF-C and sVEGFR-2) 12
  1. ALK, anaplastic lymphoma kinase; AUC, area under the curve; Cmax, maximum concentration; EGFR, endothelial growth factor receptor; GnRH, gonadotropin-releasing hormone; MOA, mechanisms of action; N/A, not available; PD, pharmacodynamics; PDGFR, platelet-derived growth factor receptor; PK, pharmacokinetics; VEGF, vascular endothelial growth factor; VEGFR, VEGF receptor