What are examples of CYP1A2 inhibitors?

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A number of medications from various drug classes, including some (but not all) antibiotics, selective serotonin reuptake inhibitors (SSRIs) and hormone therapies, can inhibit CYP1A2. Examples of CYP1A2 inhibitors can be found through various electronic drug information compendia

  • Several electronic resources include tables of cytochrome P450 (CYP) substrates, inhibitors, and inducers (e.g., FDA, UpToDate® Lexidrug™, Indiana University).1–3
  • It is important to be aware that drug-drug interactions may differ from one drug database to another, and from the fezolinetant approved product label information.

Fezolinetant is contraindicated in individuals using CYP1A2 inhibitors and the following concomitant moderate and strong CYP1A2 inhibitors were excluded from Phase 3 studies:4

Moderate Inhibitors

Strong Inhibitors

Etintidine (H-2 Receptor Antagonist)

Angelica root – Bai Zhi (Angelica dahurica radix) (Herbal medication)

Genistein (Food Product)

Ciprofloxacin (Antibiotic)

Hormonal Contraceptives (Oral Contraceptives)

Clinafloxacin (Antibiotic)

Idrocilamide (Muscle Relaxant)

Enoxacin (Antibiotic)

MDMA (Recreational Drug)

Fluvoxamine (SSRI)

Methoxsalen (8-methoxypsoralen) (Antipsoriatic)

Oltipraz (Cancer Chemopreventative Agent)

Mexiletine (Antiarrhythmic)

Rofecoxib (Nonsteroidal anti-inflammatory drug)

Osilodrostat (Adrenal Steroidogenesis Inhibitor)

Zafirlukast (Antiasthmatic)

Phenylpropanolamine (Vasoconstrictor)

Pipemidic Acid (Antibiotic)

Propafenone (Antiarrhythmic)

Propranolol (Alpha/Beta Adrenergic Antagonist)

Troleandomycin (Antibiotic)

Vemurafenib (Kinase Inhibitor)

Moderate CYP1A2 inhibitors were defined as area under the concentration-time curve ratio (AUCr) ≥ 2 and ≤ 5.

Strong CYP1A2 inhibitors were defined as AUCr > 5.

  1. Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers. FDA. Available at: https://www.fda.gov/drugs/drug-interactions-labeling/drug-development-and-drug-interactions-table-substrates-inhibitors-and-inducers.

  2. Lexidrug Online. Inhibitors and Inducers of Cytochrome P450 Enzymes (Lexi-Drugs). Available at: https://online.lexi.com/lco/action/home.

  3. Drug Interactions Flockhart TableTM. Indiana University. Available at: https://drug-interactions.medicine.iu.edu/MainTable.aspx.

  4. Data on file.

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