Baxdrostat
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Also known as Cin-107RO-6836191Ro6836191
Summary
Baxdrostat (CHEMBL4113975) is a phase-3 clinical-stage small molecule targeting CYP11B2; indicated across 2 conditions including hypertensive disorder and atherosclerosis.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 1 (CYP11B2)
- Indications: 2 conditions
- Clinical trials: 23
- Chemistry: 363.5 Da · C22H25N3O2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL4113975 |
| Name | Baxdrostat |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 71535962 |
| Molecular formula | C22H25N3O2 |
| Molecular weight | 363.5 |
| InChIKey | VDEUDSRUMNAXJG-LJQANCHMSA-N |
SMILES: CCC(=O)N[C@@H]1CCCC2=C1C=NC=C2C3=CC4=C(C=C3)N(C(=O)CC4)C
IUPAC name: N-[(8R)-4-(1-methyl-2-oxo-3,4-dihydroquinolin-6-yl)-5,6,7,8-tetrahydroisoquinolin-8-yl]propanamide
Also known as: Baxdrostat, Cin-107, CIN-107, RO-6836191, Ro6836191, BAXDROSTAT
Patent coverage: 9 distinct patent families (16 SureChEMBL compound mentions), from 2 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| CYP11B2 | CYP11B2 | Inhibition | 7.89 | 0.7% | P19099 |
Broader ChEMBL bioactivity targets: 2 (assay-derived). Sample: Cytochrome P450 11B1, mitochondrial, Cytochrome P450 11B2, mitochondrial.
Bioactivity
ChEMBL activities: 3 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 |
|---|---|---|---|---|---|
| CYP11B2 | 7.85 | EC50 | 14 | nM | CHEMBL_ACT_17773534 |
| CYP11B2 | 7.85 | EC50 | 14 | nM | CHEMBL_ACT_26634130 |
| CYP11B1 | 6.01 | EC50 | 980 | nM | CHEMBL_ACT_17773604 |
Target pathways
Aggregated over 1 target gene(s): CYP11B2.
Top Reactome pathways
14 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Metabolism | 1 | CYP11B2 |
| Disease | 1 | CYP11B2 |
| Mineralocorticoid biosynthesis | 1 | CYP11B2 |
| Glucocorticoid biosynthesis | 1 | CYP11B2 |
| Metabolism of steroid hormones | 1 | CYP11B2 |
| Biological oxidations | 1 | CYP11B2 |
| Cytochrome P450 - arranged by substrate type | 1 | CYP11B2 |
| Phase I - Functionalization of compounds | 1 | CYP11B2 |
| Endogenous sterols | 1 | CYP11B2 |
| Metabolism of lipids | 1 | CYP11B2 |
| Defective CYP11B2 causes CMO-1 deficiency | 1 | CYP11B2 |
| Metabolic disorders of biological oxidation enzymes | 1 | CYP11B2 |
| Diseases of metabolism | 1 | CYP11B2 |
| Metabolism of steroids | 1 | CYP11B2 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| regulation of blood volume by renal aldosterone | 1 |
| renal water homeostasis | 1 |
| C21-steroid hormone biosynthetic process | 1 |
| glucocorticoid biosynthetic process | 1 |
| mineralocorticoid biosynthetic process | 1 |
| cholesterol metabolic process | 1 |
| sterol metabolic process | 1 |
| aldosterone biosynthetic process | 1 |
| cellular response to hormone stimulus | 1 |
| cortisol metabolic process | 1 |
| cortisol biosynthetic process | 1 |
| cellular response to potassium ion | 1 |
| potassium ion homeostasis | 1 |
| sodium ion homeostasis | 1 |
| cellular response to peptide hormone stimulus | 1 |
Indications & clinical
Indications
2 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 |
|---|---|---|---|
| hypertensive disorder | 2 | MONDO:0005044 | EFO:0000537 |
| atherosclerosis | 1 | MONDO:0005311 | EFO:0003914 |
Clinical trials
Total trials: 23.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 10 |
| PHASE3 | 7 |
| PHASE2 | 6 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06268873 | PHASE3 | ACTIVE_NOT_RECRUITING | A Phase III Study to Investigate the Efficacy and Safety of Baxdrostat in Combination With Dapagliflozin on CKD Progression in Participants With CKD and High Blood Pressure. |
| NCT06677060 | PHASE3 | RECRUITING | Phase III Study Investigating Heart Failure and Cardiovascular Death With Baxdrostat in Combination With Dapagliflozin |
| NCT06742723 | PHASE3 | RECRUITING | A Phase III Renal Outcomes and Cardiovascular Mortality Study to Investigate the Efficacy and Safety of Baxdrostat in Combination With Dapagliflozin in Participants With Chronic Kidney Disease and High Blood Pressure |
| NCT07007793 | PHASE3 | RECRUITING | A Study to Assess Efficacy and Safety of Baxdrostat in Participants With Primary Aldosteronism |
| NCT06034743 | PHASE3 | COMPLETED | A Study to Investigate the Efficacy and Safety of Baxdrostat in Participants With Uncontrolled Hypertension on Two or More Medications Including Participants With Resistant Hypertension |
| NCT06168409 | PHASE3 | COMPLETED | A Study to Investigate the Effect of Baxdrostat on Ambulatory Blood Pressure in Participants With Resistant Hypertension |
| NCT06344104 | PHASE3 | COMPLETED | A Study to Investigate the Efficacy and Safety of Baxdrostat in Participants With Uncontrolled Hypertension on Two or More Medications Including Participants With Resistant Hypertension |
| NCT07222917 | PHASE2 | RECRUITING | A Phase IIb Study to Evaluate the Effect of Dapagliflozin in Combination With Baxdrostat Compared With Baxdrostat on Albuminuria in Participants With Chronic Kidney Disease and High Blood Pressure. |
| NCT04519658 | PHASE2 | COMPLETED | A Study of CIN-107 in Adults With Treatment-Resistant Hypertension (rHTN) |
| NCT05137002 | PHASE2 | COMPLETED | A Study of CIN-107 in Patients With Uncontrolled Hypertension |
| NCT05432167 | PHASE2 | COMPLETED | A Study to Evaluate CIN-107 for the Treatment of Patients With Uncontrolled Hypertension and Chronic Kidney Disease |
| NCT05459688 | PHASE2 | COMPLETED | Open-Label Extension Study of Patients Previously Enrolled in Study CIN-107-124 |
| NCT06336356 | PHASE2 | COMPLETED | A Study to Evaluate Cortisol Reserve in Response to Adrenocorticotropic Hormone (ACTH) Stimulation Test Following Baxdrostat Treatment Compared to Placebo in Participants With Uncontrolled Hypertension |
| NCT01995383 | PHASE1 | COMPLETED | A Single Ascending Dose Study Investigating the Safety, Pharmacokinetics and Pharmacodynamics of RO6836191 in Healthy Male Volunteers. |
| NCT05470725 | PHASE1 | COMPLETED | Study to Evaluate the Pharmacokinetics of CIN-107 in Subjects With Varying Degrees of Renal Function |
| NCT05500820 | PHASE1 | COMPLETED | Study With CIN-107 Following Multiple Oral Ascending Doses in Healthy Subjects |
| NCT05526690 | PHASE1 | COMPLETED | Study to Evaluate the Effect of CIN-107 on the Pharmacokinetics of the MATE Substrate, Metformin, in Healthy Subjects |
| NCT05961384 | PHASE1 | COMPLETED | Phase 1 Study to Determine the Metabolism and Clearance of Baxdrostat |
| NCT05961397 | PHASE1 | COMPLETED | Phase 1 PK Study to Evaluate the PK of CIN-107 in Subjects With Hepatic Impairment |
| NCT05966324 | PHASE1 | COMPLETED | Baxdrostat Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Study in a Japanese Population |
| NCT06194032 | PHASE1 | COMPLETED | A Study to Investigate the Effect on QTcF of Baxdrostat Compared With Placebo, Using Moxifloxacin as a Positive Control, in Healthy Participants |
| NCT06357520 | PHASE1 | COMPLETED | A Study to Investigate the Pharmacokinetics of Baxdrostat When Given Alone and in Combination With Itraconazole in Healthy Participants |
| NCT06657105 | PHASE1 | COMPLETED | A Study to Investigate the Pharmacokinetics of Ethinyl Estradiol and Levonorgestrel When Given Alone and in Combination With Baxdrostat in Healthy Females of Non-childbearing Potential |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
11 molecules share ≥1 primary target. Top 11 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| ABIRATERONE | ChEMBL + PubChem | Phase 4 (approved) | CYP11B2 |
| ETOMIDATE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| FLUCONAZOLE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| KETOCONAZOLE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| LETROZOLE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| METYRAPONE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| OSILODROSTAT | ChEMBL | Phase 4 (approved) | CYP11B2 |
| POSACONAZOLE | ChEMBL | Phase 4 (approved) | CYP11B2 |
| LORUNDROSTAT | ChEMBL | Phase 3 | CYP11B2 |
| DEXFADROSTAT | ChEMBL | Phase 2 | CYP11B2 |
| FADROZOLE | ChEMBL | Phase 2 | CYP11B2 |
Related Atlas pages
- Genes: CYP11B2
- Drugs: Abiraterone, Etomidate, Fluconazole, Ketoconazole, Letrozole, Metyrapone, Osilodrostat, Posaconazole, Lorundrostat