Relacorilant is a selective glucocorticoid receptor antagonist that reverses glucocorticoid-mediated anti-apoptotic signaling to restore chemosensitivity in platinum-resistant ovarian, fallopian tube, and primary peritoneal cancers. Originally investigated to manage the metabolic and endocrinologic complications of hypercortisolism, such as Cushing’s syndrome, its clinical utility has pivoted toward oncology as a potent sensitizing agent.
- Mechanism
- Curator reviewed · 4 references
Relacorilant is a potent and selective modulator of the glucocorticoid receptor (GR), with an inhibition constant (Ki) for receptor binding of 0.15 nM, and no measurable binding to other steroid receptors.
In ovarian carcinoma cell lines, GR activation leads to upregulation of glucocorticoid-regulated kinase 1 (SGK1) and map kinase phosphatase 1 (MKP1)/dual-specificity phosphatase 1 (DUSP1) genes. In this context, cortisol binding to the GR is immunosuppressive, decreasing the secretion of pro-inflammatory cytokines. The antagonism of GR by relacorilant may therefore indirectly activate the immune system, thereby enhancing the apoptosis and anti-tumor activity of co-administered paclitaxel.
- Primary indication
- Relacorilant is indicated in combination with nanoparticle albumin-bound paclitaxel for the treatment of adults with platinum-resistant epithelial ovarian, fallopian tube, or primary peritoneal cancer who have received one to three prior systemic treatment regimens, at...Curator reviewed · 3 structured indications
- Formula / weight
- C27H22F4N6O3S · 586.57 g/mol (avg)
- First approval
- United States, 2026
- Code names
- CORT-125134
- Brand names
Resolves to
WANIDIGFXJFFEL-SANMLTNESA-NSMILESCN1C=C(C=N1)S(=O)(=O)N1CCC2=CC3=C(C[C@@]2(C1)C(=O)C1=CC(=CC=N1)C(F)(F)F)C=NN3C1=CC=C(F)C=C1What you can answer from here — as of September 13, 2026
Which drugs share a target with Relacorilant, and which of those have an active Phase 3 trial?
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