Table 5.

Relationship between pharmacokinetics and telomerase inhibition

Patient IDDose level (mg/m2)Cmax (μg/mL)AUC (μg/mL•h)Duration of PBMC telomerase inhibitiona
102851418168 hours
1128511390624 hours
122851157708 days
153601991,50824 hours
163602071,30824 hours
183601691,696No inhibition observed
  • aPBMCs were collected at the following time points: (i) before the first dose of drug on day 1, (ii) 6 to 8 hours after the first dose, (iii) 24 (±2) hours after the first dose, (iv) before the imetelstat dose on day 8, and (v) before the imetelstat dose on day 1 of cycles 2 and 3. Duration of inhibition is determined as the last time point at which telomerase activity was absent.