> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/sitokiren-919706e4-b027-48f9-8591-75fe1dcdba63
> Record changed: 2026-10-13

# Sitokiren

Highest phase reached

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

## Development status

**Listing at source**

Listed

**Highest phase reached**

Phase 3

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

**Drug name**

Sitokiren

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

**Molecular weight**

444.54

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

**Structure (SMILES)**

COC(=O)NCCCn1nc(\[C@@H\](C)N(C(=O)\[C@H\]2CNCCO2)C2CC2)c2ccc(C)nc21

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

### Other names (20)

- sitokiren
- Sitokiren
- SITOKIREN
- sitokiren \[INN\]
- sitokiren inn
- sitokirene
- Sitokirene
- SITOKIRENE
- sitokireno
- Sitokireno
- SITOKIRENO
- sph 3127
- Sph-3127
- SPH-3127
- sph3127
- Sph3127
- SPH3127
- SPH3127 100mg
- SPH3127 50mg
- SPH3127 tablet

## Identifiers

**CAS registry numbers**

- 1399849-02-5

**ChEMBL ID**

CHEMBL4110551

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

**InChIKey**

GRTDDIZIUSADLD-CRAIPNDOSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4110551)

**PubChem compound IDs**

- 117877477

**FDA ingredient codes (UNII)**

- C2M78A9V6Z

## Regulatory information

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

## Pharmacology

### Drug classification

**Pharmacology name**

sitokiren

**Type**

Synthetic organic

**Drug name stem**

\-kiren

**Approval recorded by Guide to Pharmacology**

Yes

### Mechanisms of action (2)

- **Action**  
Inhibition

**Action type**  
Inhibitor

**Target**  
renin

**Gene symbol**  
REN

**Protein identifier**  
P00797

**Median affinity**

9.4

**Affinity units**  
pIC50
- **Mechanism**  
Renin inhibitor

**Action type**  
Inhibitor

**Target**  
Renin

**Protein identifier**  
P00797

### Open Targets mechanisms

- **Mechanism**  
Renin inhibitor

**Action type**  
Inhibitor

**Target**  
Renin

### Investigated indications (4)

- **Condition**  
Diabetic Nephropathies

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000401

**Subject identifier**  
D003928
- **Condition**  
Hypertension

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000537

**Subject identifier**  
D006973
- **Condition**  
Colitis, Ulcerative

**Highest recorded phase**  
2

**Condition identifier**  
EFO:0000729

**Subject identifier**  
D003093
- **Condition**  
Essential Hypertension

**Highest recorded phase**  
3

**Condition identifier**  
MONDO:0001134

**Subject identifier**  
D000075222

### Open Targets indications (6)

- **Condition identifier**  
EFO\_0000537

**Highest recorded phase**  
2
- **Condition identifier**  
EFO\_0000729

**Highest recorded phase**  
2
- **Condition identifier**  
HP\_0000822

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0001134

**Highest recorded phase**  
3
- **Condition identifier**  
MONDO\_0005016

**Highest recorded phase**  
2
- **Condition identifier**  
MONDO\_0005101

**Highest recorded phase**  
2

### Trial references (9)

- NCT03128138  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03128138)
- NCT03249753  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03249753)
- NCT03255993  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03255993)
- NCT03756103  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03756103)
- NCT05593562  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05593562)
- NCT05019742  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05019742)
- NCT05770609  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05770609)
- NCT05359068  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05359068)
- NCT05593575  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05593575)

## Chemical properties

**Hydrogen bond acceptors**

8

**Hydrogen bond donors**

2

**Polar surface area**

110.61

**Calculated partition coefficient (ALogP)**

1.53

**Calculated partition coefficient (XLogP)**

0.8

**Prodrug**

No

**Chirality**

Single enantiomer

**Inorganic**

No

**Rule-of-five violations**

0

**Rotatable bonds**

8

**Heavy atoms**

32

**Molecular formula**

C22H32N6O4

**Monoisotopic mass**

444.24850352

**Natural product**

No

## Evidence counts

**Recorded assays**

22

**Active assays**

4

### Active assay types

- Confirmatory

## Biological measurements

These details could not be displayed.

## Related records

### Trials (10)

- A Study of SPH3127 in the Treatment of Mild to Moderate Ulcerative Colitis
- Drug-drug Interaction Study of SPH3127
- [Efficacy and Safety of SPH3127 Tablets on Treating the Diabetic Kidney Disease](https://trialight.com/data/trial/efficacy-and-safety-of-sph3127-tablets-on-treating-the-992add01-3dae-4771-8444-217e9354173b.md)
- Evaluation of SPH3127 in Patients With Mild-to-Moderate Ulcerative Colitis
- Safety and Efficacy of SPH3127 on Treating Mild-moderate Essential Hypertension Patients
- Single Ascending Dose Study of Safety and Tolerability of SPH3127 Tablet in Chinese Healthy Volunteers
- Study on Human Mass Balance of SPH3127 Tablets
- Study to Evaluate the Efficacy and Safety of SPH3127 In Patients With Mild-moderate Essential Hypertension
- The Effect of Food Intake on the Pharmacokinetic of Single Dose SPH3127 Tablets in Chinese Health Subjects
- The Tolerability and Pharmacokinetics of Multiple Doses of SPH3127 in Chinese Healthy People

### In development for (4)

- [Diabetic kidney disease](https://trialight.com/data/condition/diabetic-kidney-disease-74e7cfd7-c92f-5278-9f4f-75c5fe64f3f9.md) Phase 2
- [Essential hypertension](https://trialight.com/data/condition/essential-hypertension-bd582df2-4596-58b0-aa00-37f10a4759d3.md) Phase 3
- [Hypertensive disorder](https://trialight.com/data/condition/hypertensive-disorder-6d786557-b9e8-5afc-80f3-89a1995f9da5.md) Phase 2
- [Ulcerative colitis](https://trialight.com/data/condition/ulcerative-colitis-afbc4579-f001-5a8a-b904-28f09f344ab5.md) Phase 2

### Targets (1)

- [REN](https://trialight.com/data/target/ren-0583f8fa-2894-58b0-88c4-9248e87248e8.md) Renin inhibitor

---

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