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Levodopa

Generic Name
Levodopa
Brand Names
Dhivy, Duodopa, Duopa, Inbrija, Parcopa, Prolopa, Rytary, Sinemet, Stalevo
Drug Type
Small Molecule
Chemical Formula
C9H11NO4
CAS Number
59-92-7
Unique Ingredient Identifier
46627O600J
Background

Levodopa is a prodrug of dopamine that is administered to patients with Parkinson's due to its ability to cross the blood-brain barrier. Levodopa can be metabolised to dopamine on either side of the blood-brain barrier and so it is generally administered with a dopa decarboxylase inhibitor like carbidopa to prevent metabolism until after it has crossed the blood-brain barrier. Once past the blood-brain barrier, levodopa is metabolized to dopamine and supplements the low endogenous levels of dopamine to treat symptoms of Parkinson's. The first developed drug product that was approved by the FDA was a levodopa and carbidopa combined product called Sinemet that was approved on May 2, 1975.

Indication

Levodopa on its own is formulated as an oral inhalation powder indicated for intermittent treatment of off episodes in Parkinson's patients who are already being treated with carbidopa and levodopa. Levodopa is most commonly formulated as an oral tablet with a peripheral dopa decarboxylase inhibitor indicated for treatment of Parkinson's disease, post-encephalitic parkinsonism, and symptomatic parkinsonism following carbon monoxide intoxication or manganese intoxication.

Associated Conditions
Paralysis agitans, Parkinson's Disease (PD), Parkinsonism, Parkinsonism post encephalitic, Restless Legs Syndrome (RLS), Advanced Motor fluctuations
Clinical Trials
Related News

InBrain Pharma Secures €1.8 Million to Industrialize Anaerobic Dopamine Production for Advanced Parkinson's Disease

• InBrain Pharma has received €1.8 million from France's "First Factory" initiative to scale up production of anaerobic dopamine (A-dopamine), a breakthrough therapy for advanced Parkinson's disease. • The company has partnered with CDMO IDD-Xpert to develop GMP-compliant manufacturing processes for A-dopamine, which enables direct brain infusion of dopamine—overcoming a 50-year scientific barrier. • Clinical batches will support Phase III trials beginning in 2026, with commercial production planned for early next decade, potentially transforming treatment for the two-thirds of advanced Parkinson's patients inadequately controlled by current therapies.

First Patients Receive Groundbreaking Autologous Stem Cell Treatment for Parkinson's Disease in Phase 1 Trial

• Mass General Brigham launches pioneering Phase 1 trial using patients' own reprogrammed stem cells to replace damaged dopamine neurons in Parkinson's disease, with three of six participants treated successfully. • The innovative treatment converts patients' blood cells into induced pluripotent stem cells (iPSCs), which are then transformed into dopamine neurons, eliminating the need for immunosuppression. • The FDA-approved trial, based on three decades of research at McLean Hospital, will monitor patients for 12 months to assess safety and potential improvements in Parkinson's symptoms.

Breakthrough Brain Infusion Therapy Shows Promise in Advanced Parkinson's Disease Treatment

InBrain Pharma has achieved a significant breakthrough in Parkinson's disease treatment through direct brain infusion of anaerobic dopamine, as published in Nature Medicine. The Phase I/II DIVE-I study demonstrated improved motor symptom control and reduced L-Dopa dosage requirements, potentially revolutionizing advanced Parkinson's disease management.

BlueRock Therapeutics' Bemdaneprocel Advances to Phase 3 for Parkinson's Disease

• BlueRock Therapeutics is initiating a Phase 3 trial, exPDite-2, for bemdaneprocel, a cell therapy for Parkinson's disease, expected to begin in the first half of 2025. • The exPDite-2 trial will enroll 102 patients with moderate Parkinson's, assessing the change in 'on' time without dyskinesia over 78 weeks compared to a sham surgery. • Bemdaneprocel aims to replace dopamine-producing neurons lost in Parkinson's, with Phase 1 data showing tolerability and encouraging trends in motor function. • The FDA granted bemdaneprocel Regenerative Medicine Advanced Therapy (RMAT) designation, potentially accelerating its development and review process.

Dopamine's Surprising Breakthrough in Alzheimer's Treatment

Scientists at Japan’s RIKEN Center for Brain Science have discovered a potential link between dopamine and Alzheimer’s disease, suggesting that dopamine could help break down beta-amyloid plaques, a hallmark of Alzheimer’s. This finding could lead to new treatments using existing medications like L-DOPA, offering hope for more effective management of the disease.

Novel Intracerebroventricular A-dopamine Treatment Shows Promise for Parkinson's Disease Complications

A groundbreaking clinical trial demonstrates that continuous intracerebroventricular (i.c.v.) infusion of anaerobic dopamine is both safe and effective for Parkinson's disease patients experiencing complications from traditional treatments. The study showed significant reduction in medication side effects without inducing dyskinesia, potentially offering a superior alternative to existing therapies.

FDA Approves AbbVie's Vyalev for Advanced Parkinson's Disease

• The FDA has approved AbbVie's Vyalev (foscarbidopa and foslevodopa) as a 24-hour subcutaneous infusion for motor fluctuations in advanced Parkinson's disease. • Vyalev is the first and only levodopa-based therapy delivered as a continuous 24-hour infusion, offering a non-surgical treatment option for patients. • Clinical trials showed Vyalev significantly increased "on" time without troublesome dyskinesia and decreased "off" time compared to oral carbidopa/levodopa. • The most common adverse reactions were infusion site events, hallucinations, and dyskinesia, with Medicare coverage expected in the second half of 2025.

DOD Grant Funds Research into Neuropsychiatric Symptoms of Parkinson's Disease

• A collaborative research team received a $3 million grant from the Department of Defense to investigate the neuropsychiatric symptoms of Parkinson's disease. • The research aims to understand how changes in serotonin-producing neurons contribute to cognitive, sleep, and psychiatric issues in Parkinson's patients. • Researchers are exploring how L-DOPA, a common Parkinson's treatment, affects serotonin neurons and leads to uncontrolled dopamine release and side effects. • The team has identified potential medications for repurposing to treat serotonin dysfunction in Parkinson's, with access to a large patient population for clinical trials.

Vimgreen Completes Enrollment in Phase 2 Trial of VG081821AC for Parkinson's Disease

• Vimgreen Pharmaceuticals has completed enrollment of 150 participants in a Phase 2 trial of VG081821AC for early-to-mid stage Parkinson's disease. • The trial is a 12-week, multicenter, randomized, double-blind, placebo-controlled study evaluating VG081821AC as a monotherapy. • VG081821AC, a novel adenosine A2A receptor antagonist and inverse agonist, aims to improve motor symptoms and potentially modify disease progression. • The primary endpoint is the change from baseline in MDS-UPDRS Part III score, with trial completion expected in November.

Intracerebroventricular Anaerobic Dopamine Reduces L-DOPA Complications in Parkinson's Disease

• Continuous intracerebroventricular administration of anaerobic dopamine (A-dopamine) shows promise in reducing L-DOPA-related complications (LDRC) in Parkinson's disease patients. • A phase I/IIb study demonstrated that A-dopamine significantly reduced dyskinesias and “off” periods, while also allowing for a reduction in oral L-DOPA dosage. • The treatment was found to be safe, with the most common adverse events being nausea and drowsiness during titration, and patients requested long-term continuation in compassionate use. • These findings suggest A-dopamine could offer a substantial improvement in managing severe LDRC in Parkinson's, with a large therapeutic index.

Blood-Brain Barrier Breakthrough: Novel Delivery System Shows Promise for Brain Disease Treatment

• A new molecular Trojan horse delivery system successfully transports therapeutic proteins and genes across the blood-brain barrier, potentially revolutionizing treatment for neurological diseases. • The HIRMAb-IDUA fusion protein (valanafusp alpha) has shown positive results in human clinical trials for MPSI, demonstrating both safety and efficacy in treating this rare brain disorder. • Trojan horse liposomes enable targeted delivery of gene therapies to the brain with lower doses than viral methods, while avoiding safety concerns associated with viral vectors.
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