Drug intelligence / Profile preview

Interferon alpha-2a + Tamoxifen

Development stage
Unknown
Modality
Targeted Protein Degraders (TPDs) → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules
Administration
Subcutaneous
01

Overview

The combination of interferon alpha-2a and tamoxifen represents a therapeutic approach that has been investigated for various cancers, particularly recurrent gliomas. This combination leverages the immunomodulatory properties of interferon alpha-2a with the anti-estrogenic effects of tamoxifen. The rationale for combining these drugs is that interferon alpha-2a induces the expression of estrogen receptors, potentially increasing the sensitivity of cancer cells to tamoxifen. This combination approach has also been tested in pilot clinical trials for metastatic breast cancer. A phase II trial tested high-dose tamoxifen (initially 240 mg/m²/day, later reduced to 120 mg/m²/day) with subcutaneous interferon alpha-2a (6 × 10⁶ U three times weekly) for recurrent gliomas. However, this trial was closed early due to significant neurotoxicity observed in patients, manifesting as dizziness and unsteady gait. Of 16 evaluable patients in one study, 12 had progressive disease after one treatment cycle, 3 had stable disease, and there was one minor response.

02

Targets

ESR1 (ERα)ESR2 (ERβ)IFNAR (Immune system modulation via type I interferon receptor)SHBG (Sex hormone-binding globulin)

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