Informational only. Not medical advice.INFORMATIONAL PLATFORM ONLY — NOT MEDICAL ADVICE, DIAGNOSIS, OR TREATMENT
Informational only. Not medical advice.INFORMATIONAL PLATFORM ONLY — NOT MEDICAL ADVICE, DIAGNOSIS, OR TREATMENT
Head-to-head comparison of Clascoterone (CB-03-01) and Endoxifen — mechanism, side effects, legal status, and pricing.
Clascoterone is a non-peptide steroidal topical androgen receptor antagonist—a 17α-propionate ester of cortexolone (11-deoxycortisol). Winlevi (clascoterone 1% cream) is FDA-approved (2020) for topical treatment of acne vulgaris in patients 12 years and older. A higher-strength 5% topical solution (Breezula) has completed Phase 3 trials for male androgenetic alopecia but remains investigational for that indication. Despite established androgen-receptor binding, the FDA label states the mechanism of action for acne treatment is unknown.
Endoxifen is a non-steroidal triphenylethylene selective estrogen receptor modulator (SERM) and the active secondary metabolite of tamoxifen. It is not FDA-approved and remains investigational, studied in multiple Phase 1 and Phase 2 human trials for endocrine-refractory ER-positive breast cancer, desmoid tumors, and other hormone-receptor-positive solid tumors. Endoxifen is sold by research-chemical suppliers labeled for laboratory use only, not for human consumption.
Clascoterone (CB-03-01)
Endoxifen
Category
Legal Status
Mechanism
Side Effects
COA-verified vendors · trust score ≥70 required · single-vial price — bulk/bundle deals may be lower
Clascoterone (CB-03-01)
Endoxifen
COA corpus from Disclosed Labs — independently tested batches only.
Clascoterone (CB-03-01)
2
COAs
98.8%
Avg purity
2
Labs
Endoxifen
2
COAs
99.5%
Avg purity
2
Labs
Clascoterone is an FDA-approved prescription drug. Winlevi (clascoterone 1% cream) was approved in 2020 for topical treatment of acne vulgaris in patients 12 years of age and older, based on two identical Phase 3 RCTs (NCT02608450, NCT02608476; n=1421, ages 12+) showing IGA success rates of 18.8% and 20.9% for clascoterone vs. 8.7% and 6.6% for vehicle at Week 12. A separate, higher-strength 5% topical solution (Breezula) has completed a Phase 3 trial (SCALP2, NCT05914805, actual enrollment 762) for male androgenetic alopecia; this indication is investigational/unapproved. In hamster flank-organ models (topical antiandrogen bioassay), CB-03-01 showed strong local antiandrogenic activity—roughly 4× more potent than progesterone, ~3× more potent than flutamide, ~2× more potent than finasteride, and approximately equipotent with cyproterone acetate (Celasco et al., 2004, PMID 15646372). In rat subcutaneous injection and parabiotic rat models, no systemic antiandrogenic activity was observed, supporting a peripherally-selective (non-systemic) antiandrogen profile (Celasco et al., 2004). In human primary sebocyte cultures (in vitro), clascoterone dose-dependently suppressed lipid synthesis and inflammatory cytokine production, significantly outperforming spironolactone at inhibiting inflammatory cytokine synthesis (Rosette et al., 2019, PMID 31141847).
Key references
No FDA approval or approval in any jurisdiction; endoxifen is investigational only. Human trials: Goetz et al. 2017 Phase 1 in endocrine-refractory metastatic ER-positive breast cancer (20–160 mg/day oral, no maximum tolerated dose, 3 partial responses, clinical benefit rate 26.3%); Takebe et al. 2021 Phase 1 in gynecologic, desmoid, and hormone-receptor-positive solid tumors (20–360 mg/day, no MTD, partial responses in desmoid tumors); Alliance A011203 randomized Phase 2 found Z-endoxifen not superior to tamoxifen overall but showed PFS benefit in CDK4/6-inhibitor-naive patients (HR 0.42). Preclinical: in ovariectomized mice, oral Z-endoxifen increased cancellous and cortical bone mass; in rats, reduced bone turnover and protected against bone loss; in MCF7 xenografts, showed superior antitumor activity versus tamoxifen, letrozole, and exemestane.
Clascoterone (CB-03-01) (Cosmetic) and Endoxifen (Hormone) are in different categories and target different biological pathways. This is a common pattern in multi-compound research protocols. Researchers should monitor the biomarkers from both profiles and watch for interactions listed in each compound’s contraindications. Consult a licensed healthcare provider before combining any research compounds.
This platform provides informational tools only, not medical advice. This comparison is for educational purposes only. Consult a licensed provider.
Contraindications
Lab Testing
Key references
Disclosed Labs