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Exemestane (Aromasin)

Aromatase Inhibitororal · inferred

Steroidal (irreversible/suicidal) aromatase inhibitor. Unlike anastrozole and letrozole, exemestane permanently inactivates the aromatase enzyme, requiring new enzyme synthesis for estrogen production to resume. Half-life ~24 hours. Mildly androgenic. Less impact on lipids than non-steroidal AIs.

Projected serum levels — 12.5 mg, once daily

Exemestane (Aromasin)
Exemestane (Aromasin) modeled serum levels, 12.5 mg once daily over 15 days Population-based pharmacokinetic estimate. Steady state reached after approximately 3 days. 0 2.5 5 7.5 10 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule ≈ steady state · day 3
Exemestane (Aromasin) modeled serum levels with a loading dose of 23.1 mg, then 12.5 mg once daily The first dose is larger so levels approach steady state faster. 0 2.5 5 7.5 10 Day 0 Day 4 Day 8 Day 11 Day 15 Time on a regular schedule

Maintenance schedule: 12.5 mg once daily (oral).

Loading schedule: 23.1 mg on day 1, then 12.5 mg once daily — reaching therapeutic levels sooner.

Modeled steady state after ~3 days: peak ≈ 8.6 mg, trough ≈ 4.5 mg body load. Population-based estimate over 15 days for a 12.5 mg dose at a 70 kg reference body mass — the interactive app scales curves to your doses, timing, and body mass.

Key facts

Category
Aromatase Inhibitor
Route modeled
Oral
Model confidence
inferred
Half-life
24 h
Common dose
12.5 mg
Suggested maximum
25 mg/day
Reference dose range
12.5–25 mg (single dose)
Suggested cadence
once daily
Validated against
25 mg oral — Cmax 0.018 mg/L at 1.2 h

Documented interactions

  • contraindicated
    Efavirenz (Sustiva) + Exemestane (Aromasin) CYP induction

    Efavirenz (Sustiva) inducer of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~0.15x

  • contraindicated
    Rifampin + Exemestane (Aromasin) CYP induction

    Rifampin inducer of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~0.15x

  • danger
    Amlodipine (Norvasc) + Exemestane (Aromasin) CYP inhibition

    Amlodipine (Norvasc) reversible_inhibitor of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~2.24x

  • danger
    Ashwagandha (KSM-66) + Exemestane (Aromasin) CYP inhibition

    Ashwagandha (KSM-66) reversible_inhibitor of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~2.24x

  • danger
    Berberine + Exemestane (Aromasin) CYP inhibition

    Berberine reversible_inhibitor of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~2.24x

  • danger
    Black Seed Oil (Nigella sativa / Thymoquinone) + Exemestane (Aromasin) CYP inhibition

    Black Seed Oil (Nigella sativa / Thymoquinone) reversible_inhibitor of CYP3A4 predicted to change Exemestane (Aromasin) AUC by ~2.24x

Serum checks 108 modeled interaction pairings for exemestane (aromasin) across your whole stack — absorption conflicts, enzyme inhibition, and nutrient depletion included.

Research behind this entry

  1. Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males Mauras N et al. · Journal of Clinical Endocrinology & Metabolism, 2003 DOI

    Phase I study showing 25 mg exemestane achieved peak levels at 1 hour, terminal half-life of 8.9 hours, and maximal estradiol suppression of 62% at 12 hours in young males.

  2. A Predictive Model for Exemestane Pharmacokinetics/Pharmacodynamics Incorporating the Effect of Food and Formulation Pinto N et al. · British Journal of Clinical Pharmacology, 2005 DOI

    Developed PK/PD model showing food increases exemestane bioavailability but differences in absorption do not translate to differences in pharmacodynamic estradiol suppression.

  3. An Overview of the Pharmacology and Pharmacokinetics of the Newer Generation Aromatase Inhibitors Anastrozole, Letrozole, and Exemestane Buzdar AU · Cancer, 2002 DOI

    Comparative review showing exemestane as an irreversible steroidal AI with distinct mechanism from reversible non-steroidal AIs, achieving >95% aromatase inhibition.

3 published studies referenced in the app, each with a plain-language summary.