An oral robotic pill reliably and safely delivers teriparatide with high bioavailability in healthy volunteers: A phase 1 study

摘要

Aims The incidence of osteoporosis is projected to exceed 70 million people over the age of 65 years by 2030. Osteoanabolic agents, such as teriparatide and abaloparatide, are not only effective in reducing fracture incidence but also improve skeletal microstructure—an important need not met by antiresorptive agents. However, anabolic agents must be administered by daily subcutaneous injections which can be a challenge in older women. To address this need, we have developed an oral robotic pill (RP) designed to deliver biotherapeutics safely and painlessly. Methods This report describes the results of a 2‐part Phase 1 study conducted to evaluate the safety, tolerability and pharmacokinetics of single (Part 1) and repeat doses (Part 2) of teriparatide delivered via the RP (RT‐102) in healthy and postmenopausal women. Results Teriparatide, administered by the RP, was measurable in 26/29 and 63/69 of participants in Part 1 and Part 2, respectively. RT‐102 at the 20‐μg dose yielded a lower maximum observed serum concentration (98 ± 10 vs . 128 ± 20 pg mL −1 ), delayed time to reach maximum observed serum concentration (68 ± 15 vs . 13 ± 2 min) and higher area under the curve to infinity (342 ± 44 vs . 126 ± 29 h pg mL −1 ) resulting in a 3‐fold higher bioavailability than subcutaneous injection. RT‐102 was well tolerated with only 5 mild to moderate adverse events (AEs) related to the RP that resolved without intervention and no serious AEs. Drug‐related AEs were similar in severity and frequency between RT‐102 and subcutaneous teriparatide. Conclusion These data demonstrate that RT‐102 can safely and reliably deliver therapeutic levels of teriparatide. Clinicaltrials.gov NCT#05164614.