Independent reference & toolkit 100 compounds graded · Last reviewed June 2026

Category · Aromatase inhibitors

Aromatase inhibitors: approved & repurposed.

Drugs that block the enzyme converting testosterone to estradiol — approved for breast cancer adjuvant therapy, with decades of large RCTs behind that use, and widely repurposed for estrogen management on testosterone protocols.

Two flavors. Anastrozole and letrozole are non-steroidal (they bind reversibly and block the active site). Exemestane is steroidal (it binds irreversibly and the enzyme has to be re-synthesized). That difference shows up clinically: exemestane crashes estrogen harder but has a gentler effect on lipids; non-steroidals are easier to titrate but tank HDL more aggressively at full doses.

Important: the FDA-approved indications (post-menopausal breast cancer adjuvant) sit at grade 10. Off-label use for estrogen management on enhanced protocols is the default in many communities but is much more sparsely studied — judge expectations accordingly.

Evidence spread
10 · Established 3
The aromatase inhibitors 3

Reading this class honestly

AIs are easy to over-use. Crashed estrogen — joint pain, libido, lipid harm — is one of the most common preventable problems on cycle. The bloodwork tool flags E2 below 12 as classic over-suppression when an AI is in play. See how we grade for the 1–10 logic.