Parathyroid hormone (1-34)-coated microneedle patch system: clinical pharmacokinetics and pharmacodynamics for treatment of osteoporosis

Pharm Res. 2011 Jan;28(1):159-65. doi: 10.1007/s11095-010-0192-9. Epub 2010 Jun 22.


Objectives: To evaluate the clinical PK/PD of PTH(1-34) delivered by a novel transdermal drug-coated microneedle patch system (ZP-PTH) for the treatment of osteoporosis.

Methods: Phase 1 PK studies evaluated the effect of site of administration, patch wear time and dose in normal volunteers, ages 40-85 yrs. Phase 2 was conducted in post-menopausal women with osteoporosis to determine the patch dose response compared to placebo patch and FORTEO® injection.

Results: Phase 1 ZP-PTH patch delivery demonstrated a rapid PTH plasma pulse profile with T(max) 3 times shorter and apparent T(1/2) 2 times shorter than FORTEO®. In Phase 2, ZP-PTH 20, 30 and 40 µg doses showed a proportional increase in plasma PTH AUC. Inter-subject and intra-subject AUC variability was similar for all patch doses and comparable to injection. All patch doses produced a significant increase in spine bone mineral density. Unexpectedly, ZP-PTH also produced an early increase in hip bone mineral density, an effect not observed with the injection.

Conclusions: These studies suggest that this novel ZP-PTH patch system can deliver a consistent and therapeutically relevant PTH PK profile. Based on encouraging Phase 2 safety and efficacy data, the program is advancing into a pivotal Phase 3 clinical study.

Publication types

  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Bone Density Conservation Agents* / administration & dosage
  • Bone Density Conservation Agents* / pharmacokinetics
  • Bone Density Conservation Agents* / therapeutic use
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Drug Delivery Systems / adverse effects
  • Drug Delivery Systems / instrumentation
  • Drug Delivery Systems / methods*
  • Equipment Design
  • Female
  • Humans
  • Injections, Intradermal
  • Microinjections / adverse effects
  • Microinjections / instrumentation
  • Microinjections / methods*
  • Middle Aged
  • Needles*
  • Osteoporosis, Postmenopausal / drug therapy*
  • Teriparatide* / administration & dosage
  • Teriparatide* / pharmacokinetics
  • Teriparatide* / therapeutic use
  • Time Factors
  • Tissue Distribution
  • Treatment Outcome


  • Bone Density Conservation Agents
  • Teriparatide