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ba0003pp6 | Arthritis and other joint diseases: translational and clinical | ECTS2014

MIV-711, a highly selective cathepsin K inhibitor: safety, pharmacokinetics and pharmacodynamics of multiple oral doses in healthy postmenopausal women

Grabowska Urszula , Lindstrom Erik , Jerling Markus , Edenius Charlotte

Introduction: Cathepsin K is necessary for bone matrix resorption. Excessive resorption associated with osteoporosis and osteoarthritis can be reduced by cathepsin K inhibition. MIV-711, a highly selective cathepsin K inhibitor, successfully attenuates both bone resorption and cartilage degradation in non-clinical studies.Aim: To determine safety, tolerability, pharmacokinetics and pharmacodynamics of MIV-711 during multiple oral dosing to postmenopausal...

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ba0001pp225 | Cell biology: osteoclasts and bone resorption | ECTS2013

Inhibition of lipopolysacharide induced osteoclast formation and bone resorption in vitro and in vivo in mice by cystatin C

Fredrik Stralberg , Lindholm Catharina , Lindstrom Erik , Kasprzykowski Franciszek , Saftig Paul , Abrahamson Magnus , Grubb Anders , Lerner Ulf H

RANKL induced osteoclastogenesis is mediated by several transcription factors such as NF-κB, AP-1 and Nfatc1. We have found that also cysteine proteinases are involved in the signaling pathway downstream RANK. Thus, cystatin C, Z-RLVG-CHN2 (the sequence of which is based upon one of the enzyme inhibitory domains in cystatin C) and the fungal molecule E-64 inhibit RANKL induced mouse and human osteoclast formation in vitro (Strålberg et ...

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ePoster

ba0001pp430 | Osteoporosis: treatment | ECTS2013

First in man study of a novel and highly selective cathepsin K inhibitor miv-711 – safety, pharmacokinetics and pharmacodynamics of single ascending oral doses in healthy subjects

Grabowska Urszula , Lindstrom Erik , Jerling Markus , Larsson Torbjorn , Bottiger Disa , Danielson Kerstin , Kristensen Jens D , Edenius Charlotte

Aim: To determine the safety, tolerability, pharmacokinetics and pharmacodynamics of the cathepsin K inhibitor MIV-711.Methods: A double-blind, placebo-controlled, randomized study in 27 healthy subjects of both genders. Single ascending doses 20600 mg were investigated for adverse events, clinical chemistry, vital signs, ECG parameters, pharmacokinetics, and serum levels of CTX-I.Results: MIV-711 was well tolerated with no a...

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Bone Abstracts

MIV-711, a highly selective cathepsin K inhibitor: safety, pharmacokinetics and pharmacodynamics of multiple oral doses in healthy postmenopausal women

Inhibition of lipopolysacharide induced osteoclast formation and bone resorption in vitro and in vivo in mice by cystatin C

First in man study of a novel and highly selective cathepsin K inhibitor miv-711 – safety, pharmacokinetics and pharmacodynamics of single ascending oral doses in healthy subjects

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