Joshua T Myers, Alyson Yamaguchi, April Toledo Vo, Anvesh Dasari, Archana Battiwala, Nidhi Patel, Leonard C Fung, Ofer M Gonen, Mir Imran, Jacques Van Dam, Mir A Hashim, Arvinder K Dhalla, John P Bilezikian
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引用次数: 0
Abstract
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.
期刊介绍：
Published on behalf of the British Pharmacological Society, the British Journal of Clinical Pharmacology features papers and reports on all aspects of drug action in humans: review articles, mini review articles, original papers, commentaries, editorials and letters. The Journal enjoys a wide readership, bridging the gap between the medical profession, clinical research and the pharmaceutical industry. It also publishes research on new methods, new drugs and new approaches to treatment. The Journal is recognised as one of the leading publications in its field. It is online only, publishes open access research through its OnlineOpen programme and is published monthly.
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