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all-trans retinoic acid + mifepristone + tamoxifen + cannabidiol
- Development stage
- Unknown
- Lead developer
- Mahmoud Ramadan mohamed Elkazzaz
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
This investigational quadrate combination therapy, developed by Mahmoud Ramadan Mohamed Elkazzaz, is being evaluated for the treatment of early breast cancer. The regimen consists of all-trans retinoic acid (ATRA), mifepristone (an antiprogesterone), tamoxifen (a selective estrogen receptor modulator), and cannabidiol (acting as a selective CYP26 inhibitor). The therapeutic rationale is based on preventing the induction of therapy-resistant cytokeratin 5 (CK5)-expressing cancer stem cells, which are often expanded by progesterone or standard hormonal treatments. In this protocol, mifepristone counteracts the progesterone-mediated induction of CK5+ cells, while cannabidiol is included to inhibit CYP26 enzymes, thereby preventing the degradation of retinoic acid and potentially enhancing its anti-tumor activity. Additionally, cannabidiol acts as an atypical inhibitor of CYP2D6 to modulate the metabolic profile of the combination.
- Other names
- Quadrate combination therapyMifepristone + Tamoxifen + Retinoic acid + CannabidiolATRA + Mifepristone + Tamoxifen + Cannabidiol
02
Targets
RARA (Retinoic acid receptor alpha)PR (Progesterone receptor)ESR1 (ERα)CYP2D6 (Cytochrome P450 2D6)GR (Glucocorticoid receptor)ESR2 (ERβ)RARG (Retinoic acid receptor gamma)RARB (Retinoic acid receptor beta)CYP26A1 (Cytochrome P450 26A1)
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