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ZA

Merck Sharp & Dohme LLC · FDA-approved active Small molecule

ZA is a bisphosphonate that inhibits bone resorption by suppressing osteoclast activity and promoting osteoclast apoptosis.

ZA is a bisphosphonate that inhibits bone resorption by suppressing osteoclast activity and promoting osteoclast apoptosis. Used for Multiple myeloma with bone disease, Metastatic bone disease in solid tumors, Hypercalcemia of malignancy.

At a glance

Generic nameZA
Also known asZometa®
SponsorMerck Sharp & Dohme LLC
Drug classBisphosphonate
TargetFarnesyl pyrophosphate synthase (indirect); hydroxyapatite in bone (binding site)
ModalitySmall molecule
Therapeutic areaOncology, Bone Metabolism
PhaseFDA-approved

Mechanism of action

Bisphosphonates like zoledronic acid (ZA) bind to hydroxyapatite in bone and are internalized by osteoclasts during bone resorption. Once inside osteoclasts, they inhibit farnesyl pyrophosphate synthase in the mevalonate pathway, disrupting the prenylation of small GTPases essential for osteoclast function and survival. This leads to osteoclast apoptosis and reduced bone turnover.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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