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AFQ056 with L-dopa

Novartis · Phase 2 active Small molecule

AFQ056 is a metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator that reduces excessive glutamatergic signaling, combined with L-dopa to enhance dopaminergic activity in Parkinson's disease.

AFQ056 is a metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator that reduces excessive glutamatergic signaling, combined with L-dopa to enhance dopaminergic activity in Parkinson's disease. Used for Parkinson's disease with motor complications (dyskinesias and motor fluctuations).

At a glance

Generic nameAFQ056 with L-dopa
SponsorNovartis
Drug classmGluR5 negative allosteric modulator
TargetmGluR5 (metabotropic glutamate receptor 5)
ModalitySmall molecule
Therapeutic areaNeurology
PhasePhase 2

Mechanism of action

AFQ056 selectively blocks mGluR5 receptors on the postsynaptic side of glutamatergic synapses, reducing excitotoxic glutamate signaling that contributes to motor complications in Parkinson's disease. When combined with L-dopa (levodopa), the mGluR5 inhibition may enhance dopaminergic efficacy and reduce dyskinesias and motor fluctuations. This combination approach targets both the dopamine deficit and the secondary glutamatergic dysfunction characteristic of advanced Parkinson's disease.

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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