Last reviewed 2026-04-19 · How we verify

DIAZOXIDE CHOLINE

12.1 Mechanism of Action The exact mechanism of action of diazoxide choline in the treatment of hyperphagia in patients 4 years of age and older with Prader-Willi syndrome (PWS) is unknown.

At a glance

Mechanism of action

1 INDICATIONS AND USAGE VYKAT XR is indicated for the treatment of hyperphagia in adults and pediatric patients 4 years of age and older with Prader-Willi syndrome (PWS). VYKAT XR is indicated for the treatment of hyperphagia in adults and pediatric patients 4 years of age and older with Prader-Willi syndrome (PWS). ( 1 )

Approved indications

No approved indications tracked.

Common side effects

No common side effects on file.

Drug interactions

• 7 DRUG INTERACTIONS Table 4 displays clinically significant drug interactions with VYKAT XR. Table 4: Clinically Significant Drug Interactions with VYKAT XR Strong CYP1A2 Inhibitors See www.fda.gov/CYPandTransporterInteractingDrugs for examples of strong CYP1A2 and CYP3A4 inhibitors, sensitive CYP1A2 substrates, and dual strong CYP3A4 / moderate 1A2 inducers. Prevention or Management Reduce the dosage of VYKAT XR when concomitantly used with strong inhibitors of CYP1A2 [see Dosage and Administration (2.4) ] . Mechanism and Clinical Effect(s) VYKAT XR is a CYP1A2 substrate. Concomitant use of VYKAT XR with strong CYP1A2 inhibitors increases exposure of diazoxide, which may increase the frequency and/or severity of adverse reactions from VYKAT XR [see Clinical Pharmacology (12.3) ] . CYP1A2 Substrates Prevention or Management Concomitant use of VYKAT XR with CYP1A2 substrates is not recommended. Mechanism and Clinical Effect(s) VYKAT XR is an inhibitor of CYP1A2. Concomitant use of VYKAT XR with CYP1A2 substrates increases exposure of these substrates. This may increase the frequency and/or severity of adverse reactions from such substrates. Strong CYP3A4 Inhibitors Prevention or Management Monitor the frequency and severity of adverse reactions from VYKAT XR. A dosage reduction of VYKAT XR may be needed when used concomitantly with strong CYP3A4 inhibitors. Mechanism and Clinical Effect(s) Concomitant use of VYKAT XR with strong CYP3A4 inhibitors increases exposure of diazoxide, which may increase the frequency and/or severity of adverse reactions from VYKAT XR [see Clinical Pharmacology (12.3) ] . Dual Strong CYP3A4 / Moderate 1A2 Inducers Prevention or Management Concomitant use of VYKAT XR with dual strong CYP3A4/moderate CYP1A2 inducers is not recommended. Mechanism and Clinical Effect(s) VYKAT XR is a substrate of CYP3A4 and CYP1A2. Concomitant use of VYKAT XR with strong CYP3A4/moderate 1A2 inducers may decrease exposure of VYKAT XR. This may decrease the efficacy of VYKAT XR [see Clinical Pharmacology (12.3) ] . Drugs Highly Bound to Protein Prevention or Management Monitor international normalized ratio (INR) in patients who use coumarin or its derivatives concomitantly with VYKAT XR. Dosage modification of coumarin or its derivatives may be needed when used concomitantly with VYKAT XR. Monitor diphenylhydantoin serum levels when VYKAT XR is used concomitantly with diphenylhydantoin. Dosage modification of diphenylhydantoin may be needed when used concomitantly with VYKAT XR. Mechanism and Clinical Effect(s) Diazoxide is highly bound to serum proteins. Diazoxide may displace other drugs which are also highly bound to protein resulting in higher or lower blood levels of the concomitantly used drugs. The impact of protein binding displacement is expected to be clinically important for drugs with narrow therapeutic range such as coumarin or its derivatives and diphenylhydantoin. Protein binding displacement may result in an increased risk of adverse reactions due to higher blood levels of coumarin or its derivative or loss of efficacy due to lower exposures of diphenylhydantoin. Thiazide or Other Diuretics Prevention or Management Monitor for signs and symptoms of hyperglycemia [see Warnings and Precautions (5.1) ] and hyperuricemia when VYKAT XR is used concomitantly with thiazides or other diuretics. Dosage adjustment of VYKAT XR or diuretics may be needed when VYKAT XR is concomitantly used with diuretics. Mechanism and Clinical Effect(s) Both diazoxide and thiazides or other diuretics may produce hyperglycemia and hyperuricemia. The concomitant use of VYKAT XR with thiazides or other diuretics may potentiate the hyperglycemic and hyperuricemic effects of diazoxide [see Adverse Reactions (6) and Clinical Pharmacology (12.2) ] . Strong CYP1A2 Inhibitors: Reduce VYKAT XR dosage. ( 2.4 , 7 ) CYP1A2 Substrates: Concomitant use with VYKAT XR is not recommended. ( 7 ) See full prescribing information for additional clinically

Key clinical trials

• An Open-Label Study of Diazoxide Choline Controlled-Release Tablet in Patients With Prader-Willi Syndrome (Phase 3)
• A Multi-Center, Randomized, Double-Blind, Placebo-Controlled Study Assessing the Efficacy, Safety and Tolerability of Diazoxide Choline Controlled-Release Tablet (DCCR) in Subjects Without Diabetes Me (Phase 2)
• A Randomized, Open-label, Multi-dose Crossover Study Assessing the Pharmacokinetic Profiles of Diazoxide Choline Coated Versus Uncoated Formulations in Healthy Volunteers (Phase 1)
• A Randomized, Open-Label, Single- and Multiple-Dose, Four-Way Parallel Study Comparing the Fed and Fasted Pharmacokinetics of Two Dose Levels of Diazoxide Choline Controlled-Release Tablet (DCCR) in H (Phase 1)
• A Dose Titration Study of Diazoxide Choline Controlled-Release Tablet (DCCR) in Patients With Prader-Willi Syndrome With a Double-Blind, Placebo-Controlled, Randomized Withdrawal Extension (Phase 1)
• A Randomized, Double-Blind, Placebo-Controlled Study Assessing the Efficacy and Safety of Diazoxide Choline in Non-Diabetic Hypertriglyceridemic Subjects (Phase 2)
• An Open-Label Study of DCCR (Diazoxide Choline) Extended-Release Tablets in Patients With Prader-Willi Syndrome (Phase 3)
• A Randomized, Double-Blind, Placebo-Controlled Study of Diazoxide Choline Controlled-Release Tablet (DCCR) in Patients With Prader-Willi Syndrome (Phase 3)

Patents

Primary sources

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