Icaritin
drugOn this page
Also known as SGN-162SGN162
Summary
Icaritin (CHEMBL498485) is a phase-3 clinical-stage small molecule; indicated across 3 conditions including hepatocellular carcinoma and neoplasm.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Indications: 3 conditions
- Clinical trials: 12
- Chemistry: 368.4 Da · C21H20O6
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL498485 |
| Name | Icaritin |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 5318980 |
| Molecular formula | C21H20O6 |
| Molecular weight | 368.4 |
| InChIKey | TUUXBSASAQJECY-UHFFFAOYSA-N |
SMILES: CC(=CCC1=C2C(=C(C=C1O)O)C(=O)C(=C(O2)C3=CC=C(C=C3)OC)O)C
IUPAC name: 3,5,7-trihydroxy-2-(4-methoxyphenyl)-8-(3-methylbut-2-enyl)chromen-4-one
Also known as: Icaritin, SGN-162, SGN162, ICARITIN
Patent coverage: 449 distinct patent families (700 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 583 (83%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: cGMP-specific 3’,5’-cyclic phosphodiesterase, Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase, Lysine-specific histone demethylase 1A.
Bioactivity
ChEMBL activities: 1 potent at pChembl ≥ 5 of 3 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| PDE5A | 5.66 | IC50 | 2200 | nM | CHEMBL_ACT_2232589 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
Clinical trials
Total trials: 12.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 5 |
| PHASE3 | 3 |
| PHASE1 | 2 |
| PHASE1/PHASE2 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05594927 | PHASE3 | RECRUITING | Icaritin Soft Capsule Versus Huachansu Tablet in the First-line Treatment of Unresectable Hepatocellular Carcinoma With Poor Conditions and Biomarker Enrichment (Biomarker Enrichment Study of Poor Prognosis HCC Patients, BESTPOP) |
| NCT03236636 | PHASE3 | UNKNOWN | The Phase III Study of Icaritin Versus HUACHANSU PIAN in Hepatocellular Carcinoma Subjects |
| NCT03236649 | PHASE3 | TERMINATED | The Phase III Study of Icaritin Versus Sorafenib in PD-L1 Positive Advanced Hepatocellular Carcinoma Subjects |
| NCT06825546 | PHASE2 | RECRUITING | Icaritin in Combination With AG in Patients With Previously Untreated Advanced Pancreatic Ductal Adenocarcinoma |
| NCT06896396 | PHASE1/PHASE2 | NOT_YET_RECRUITING | Icaritin Soft Capsules+TACE+Immunotherapy+Targeted Therapy Versus TACE+Immunotherapy+Targeted Therapy for Unresectable Hepatocellular Carcinoma |
| NCT07328828 | PHASE2 | ACTIVE_NOT_RECRUITING | Single-Arm Clinical Study of Icaritin Soft Capsules as Adjuvant Therapy for Hepatocellular Carcinoma Patients at High Risk of Postoperative Recurrence |
| NCT01972672 | PHASE2 | COMPLETED | The Phase II Study of Icaritin in Patients With Advanced Hepatocellular Carcinoma |
| NCT05903456 | PHASE2 | UNKNOWN | Icaritin Soft Capsule Combined With Lenvatinib and TACE for the Treatment of Hepatocellular Carcinoma |
| NCT06285149 | PHASE2 | UNKNOWN | Tace With Icaritin in First-line Treatment of Middle and Advanced HCC in Child Grade B Patients |
| NCT01278810 | PHASE1 | UNKNOWN | Phase I Study of Novel Estrogen Receptor(ER) a36 Modifier Icaritin in Advanced Breast Cancer Patients |
| NCT02496949 | PHASE1 | COMPLETED | A Phase Ib Study to Assess Safety and Efficacy of Oral Icaritin in Advanced Solid Tumors |
| NCT06893887 | Not specified | RECRUITING | Individualized Comprehensive Treatment for Advanced Hepatocellular Carcinoma |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).
Related Atlas pages
- Diseases: hepatocellular carcinoma