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Drug Interactions between momelotinib and Rifadin IV

This report displays the potential drug interactions for the following 2 drugs:

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Interactions between your drugs

Minor

rifAMPin momelotinib

Applies to: Rifadin IV (rifampin) and momelotinib

Coadministration with rifampin may alter the plasma concentrations and effects of momelotinib. Rifampin is an acute inhibitor of the hepatic uptake transporters organic anion transporting polypeptides (OATP) 1B1 and/or 1B3 but this is followed by potent induction of CYP450 3A4 after multiple dosing. Momelotinib is a substrate of both OATP1B1/1B3 and CYP450 3A4. In a phase I study, coadministration of momelotinib (200 mg) with a single dose of rifampin (600 mg) increased the peak plasma concentration (Cmax) and systemic exposure (AUC) of momelotinib by 40% and 57%, respectively. The Cmax and AUC of its active metabolite, M21, increased by 6% and 12%, respectively. However, the net effect after coadministration of multiple doses of rifampin (600 mg) when compared to momelotinib alone was a reduction in the momelotinib AUC by 15% and no change to its Cmax. Therefore, due to the potentially opposing effects by rifampin of OATP 1B1/1B3 inhibition and CYP450 3A4 induction, the effect of multiple doses of rifampin on momelotinib pharmacokinetics compared with momelotinib alone does not appear to be clinically significant.

References (9)
  1. (2023) "Product Information. Ojjaara (momelotinib)." GlaxoSmithKline
  2. (2024) "Product Information. Omjjara (momelotinib)." GlaxoSmithKline Australia Pty Ltd
  3. (2024) "Product Information. Ojjaara (momelotinib)." GlaxoSmithKline Inc
  4. Ho YL, Gorycki P, Ferron-Brady G, Martin P, Vlasakakis G (2024) "Clinical assessment of momelotinib drug-drug interactions via CYP3A metabolism and transporters" Clin Transl Sci, 17, p. 1-14
  5. Schilling U, Dingemanse J, Voors-Pette C, Romeijn C, Dogterom P, Ufer M (2020) "Effect of Rifampin Mediated OATP1B1 and OATP1B3 Transporter Inhibition on the Pharmacokinetics of the P2Y12 Receptor Antagonist Selatogrel" Clin Transl Sci, 13, p. 886-890
  6. Mori D, Kimoto E, Rago B, kondo y, King-Ahmad A, Ragu R, Wood LS, Johnson JG, Le VH, Vourvahis M, David Rodrigues A, Muto C, furihata k, Sugiyama Y (2020) "Dose Dependent Inhibition of OATP1B by Rifampicin in Healthy Volunteers: Comprehensive Evaluation of Candidate Biomarkers and OATP1B Probe Drugs" Clin Pharmacol Ther, 107, p. 1004-1013
  7. Lau YY, Huang Y, frassetto l, Benet LZ (2007) "Effect of OATP1B Transporter Inhibition on the Pharmacokinetics of Atorvastatin in Healthy Volunteers" Clin Pharmacol Ther, 81, p. 194-204
  8. reitman m, Chu X, Cai X, Yabut J, Venkatasubramanian R, Zajic R, Stone J, Ding Y, Witter R, Gibson C, Roupe K, Evers R, Wagner J, Stoch A (2011) "Rifampin's Acute Inhibitory and Chronic Inductive Drug Interactions: Experimental and Model-Based Approaches to Drug-Drug Interaction Trial Design" Clin Pharmacol Ther, 89, p. 234-242
  9. (2025) "Product Information. Omjjara (momelotinib)." GlaxoSmithKline UK Ltd

Drug and food interactions

Moderate

rifAMPin food

Applies to: Rifadin IV (rifampin)

GENERALLY AVOID: Concurrent use of rifampin in patients who ingest alcohol daily may result in an increased incidence of hepatotoxicity. The increase in hepatotoxicity may be due to an additive risk as both alcohol and rifampin are individually associated with this adverse reaction. However, the exact mechanism has not been established.

ADJUST DOSING INTERVAL: Administration with food may reduce oral rifampin absorption, increasing the risk of therapeutic failure or resistance. In a randomized, four-period crossover phase I study of 14 healthy male and female volunteers, the pharmacokinetics of single dose rifampin 600 mg were evaluated under fasting conditions and with a high-fat meal. Researchers observed that administration of rifampin with a high-fat meal reduced rifampin peak plasma concentration (Cmax) by 36%, nearly doubled the time to reach peak plasma concentration (Tmax) but reduced overall exposure (AUC) by only 6%.

MANAGEMENT: The manufacturer of oral forms of rifampin recommends administration on an empty stomach, 30 minutes before or 2 hours after meals. Patients should be encouraged to avoid alcohol or strictly limit their intake. Patients who use alcohol and rifampin concurrently or have a history of alcohol use disorder may require additional monitoring of their liver function during treatment with rifampin.

References (6)
  1. (2022) "Product Information. Rifampin (rifAMPin)." Akorn Inc
  2. (2022) "Product Information. Rifampicin (rifampicin)." Mylan Pharmaceuticals Inc
  3. (2023) "Product Information. Rifadin (rifampicin)." Sanofi
  4. (2024) "Product Information. Rifadin (rifaMPICin)." Sanofi-Aventis Australia Pty Ltd
  5. Peloquin CA, Namdar R, Singleton MD, Nix DE (2024) Pharmacokinetics of rifampin under fasting conditions, with food, and with antacids https://pubmed.ncbi.nlm.nih.gov/9925057/
  6. (2019) "Product Information. Rofact (rifampin)." Bausch Health, Canada Inc.

Therapeutic duplication warnings

No warnings were found for your selected drugs.

Therapeutic duplication warnings are only returned when drugs within the same group exceed the recommended therapeutic duplication maximum.

See also

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Drug Interaction Classification

These classifications are only a guideline. The relevance of a particular drug interaction to a specific individual is difficult to determine. Always consult your healthcare provider before starting or stopping any medication.
Major Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
Unknown No interaction information available.

Further information

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