High Purity 99% White Powder Sodium Dichloroacetate CAS 2156-56-1 DCA Anticancer

Sodium Dichloroacetate More Info

Sodium dichloroacetate (DCA) is a small molecule and the sodium salt of dichloroacetic acid, known for its ability to modulate cellular metabolism by targeting mitochondrial function.

Mechanism of Action

DCA primarily acts by inhibiting pyruvate dehydrogenase kinase (PDK), an enzyme that phosphorylates and inactivates the pyruvate dehydrogenase complex (PDC). By inhibiting PDK, DCA reactivates PDC, which promotes the conversion of pyruvate to acetyl-CoA, thereby enhancing mitochondrial oxidative phosphorylation and reducing lactate production. This shift restores normal cellular respiration and energy metabolism, particularly in cells with dysfunctional mitochondria or altered metabolism such as cancer cells, cells in pulmonary arterial hypertension, chronic fatigue syndrome, and endometriosis.

Applications

Treatment of mitochondrial disorders (genetic or acquired) for over 40 years.
Investigational use in cancer therapy to target tumor metabolism.
Potential treatment for pulmonary arterial hypertension, chronic fatigue syndrome, and endometriosis by normalizing mitochondrial function.
Experimental use in metabolic diseases involving lactic acidosis.

Dosage and Administration

Available as an oral or injectable agent.
Effects on PDK and mitochondrial function typically begin within 15–30 minutes after dosing.
Therapeutic effects last 12–24 hours, requiring regular dosing for sustained benefit.

Pharmacological Effects

Stimulates peripheral glucose utilization and inhibits gluconeogenesis, reducing hyperglycemia.
Inhibits lipogenesis and cholesterol synthesis, lowering circulating lipid levels.
Facilitates oxidation of lactate, improving conditions like congenital and acquired lactic acidosis.
Enhances cardiac output and myocardial efficiency under ischemic conditions by promoting carbohydrate and lactate metabolism over fatty acid metabolism.
May improve brain function after cerebral ischemia by enhancing regional lactate removal.

Safety and Side Effects

Common side effects:
Peripheral neuropathy (up to 20% of patients), manifesting as tingling, numbness, tremor, or pain in extremities; reversible upon dose reduction or discontinuation.
Sleepiness, mental fogginess, and confusion.
Mild gastrointestinal symptoms such as heartburn, nausea, and digestive discomfort.
Rare side effects:
Mild, asymptomatic elevations in liver enzymes.
Anxiety, mood changes, and hallucinations, especially when combined with CNS-active drugs.
Tumor site pain related to increased cancer cell apoptosis (rare).
Side effects are generally dose-dependent and more frequent in patients over 40 years old.
Peripheral neuropathy may be related to thiamine deficiency and can be mitigated with thiamine supplementation.
Most side effects resolve within days to weeks after stopping DCA.

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FAQ

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