Laroprovstat
Highest phase reached
Phase 2
Drug type
Small molecule
- Listing at source
- Listed
- Highest phase reached
- Phase 2
- Drug type
- Small molecule
- Drug name
- Laroprovstat
- Molecular weight
- 414.42
- Structure (SMILES)
- O=c1ccccn1-c1ccc(N[C@H]2CC[C@H](Nc3ncc(OC(F)F)cn3)C2)nc1
- az 14232880
- AZ-14232880
- az14232880
- AZ14232880
- azd 0780
- AZD 0780 [WHO-DD]
- azd 0780 who dd
- AZD-0780
- azd0780
- AZD0780
- AZD0780 tablet
- cr 000501656
- CR-000501656
- cr000501656
- CR000501656
- dgm 1656
- DGM-1656
- laroprovstat
- Laroprovstat
- laroprovstat [INN]
- LAROPROVSTAT [USAN]
- laroprovstat inn
- laroprovstat usan
- CAS registry numbers
- 2455427-91-3
- ChEMBL ID
- CHEMBL5404296
- InChIKey
- NCHUWRLOTSAFFN-KBPBESRZSA-N
- PubChem compound IDs
- 154653847
- FDA ingredient codes (UNII)
- 9EEL3YMY29
- First in class
- No
- Orphan designation
- No
- Pharmacology name
- laroprovstat
- Type
- Synthetic organic
- Drug name stem
- -stat
Mechanisms of action
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- proprotein convertase subtilisin/kexin type 9
- Gene symbol
- PCSK9
- Protein identifier
- Q8NBP7
- Median affinity
- 6.7
- Affinity units
- pKd
Investigated indications
- Condition
- Hyperlipidemias
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0021187
- Subject identifier
- D006949
- Condition identifier
- HP_0003124
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002525
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0021187
- Hydrogen bond acceptors
- 8
- Hydrogen bond donors
- 2
- Polar surface area
- 93.96
- Calculated partition coefficient (ALogP)
- 3.07
- Calculated partition coefficient (XLogP)
- 3.4
- Prodrug
- No
- Chirality
- Single enantiomer
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 7
- Heavy atoms
- 30
- Molecular formula
- C20H20F2N6O2
- Monoisotopic mass
- 414.16158023
- Natural product
- No
- Recorded assays
- 3
- Active assays
- 3
Active assay types
- Confirmatory
Related records
Trials (21)
- A Phase I Study Comparing the Relative Bioavailability of a Fixed-Dose Combination of Laroprovstat/Rosuvastatin vs Their Single Therapy Products in Healthy Adults
- A Phase I Study to Investigate the Effect of Renal Impairment on the Pharmacokinetics, Safety, and Tolerability of AZD0780
- A Phase I, Cross-over Study Comparing the Relative Bioavailability of Laroprovstat Plus Ezetimibe Fixed Combination Drug Products Versus Their Single Therapy Products in Healthy Adults
- A Phase III Study of AZD0780 on Major Adverse CV Events in Patients With a History of ASCVD Events or at High Risk for a First Event
- A Phase III Study to Assess the Effect of AZD0780 on LDL-C in Patients With Clinical ASCVD or at Risk for a First ASCVD Event
- A Phase III Study to Assess the Effect of AZD0780 on LDL-C in Patients With HeFH
- A Phase III Study to Assess the Effect of FDC Laroprovstat/Rosuvastatin Compared With Laroprovstat, Rosuvastatin and Placebo on LDL-C in LLT-naïve Patients.
- A Phase III Study to Assess the Effect of FDC Laroprovstat/Rosuvastatin Compared With Rosuvastatin on LDL-C in Patients With Hypercholesterolaemia
- A Study to Assess the Effect of AZD0780 on Ambulatory Blood Pressure
- A Study to Assess the Effect of AZD0780 on the Pharmacokinetics of AZD4954 and Vice Versa in Healthy Adults
- A Study to Assess the Effect of AZD0780 on the Pharmacokinetics of Rosuvastatin.
- A Study to Assess the Efficacy, Safety and Tolerability of Different Doses of AZD0780 in Patients With Dyslipidemia
- A Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of AZD0780 in Healthy Subjects
- A Study to Evaluate the Efficacy, Safety, and Pharmacokinetics of AZD0780 in Participants With Dyslipidaemia
- A Study to Investigate Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics With AZD0780 Following Repeated Dose Administration in Healthy Adults With Elevated LDL-C Levels
- A Study to Investigate the Effect of AZD0780 on Metformin Pharmacokinetics in Healthy Adult Volunteers Aged 18 to 55 Years
- A Study to Investigate the Effect of AZD0780 Tablets in Combination With Rosuvastatin Tablets on Low Density Lipoprotein Cholesterol Levels (LDL-C) in Adult Participants With Dyslipidaemia
- A Study to Investigate the Pharmacokinetics, Safety, Tolerability, and Efficacy of AZD0780 With Ezetimibe Combinations in Healthy Adults With Elevated LDL-C.
- An ADME Study of [14C]AZD0780 in Healthy Male Subjects
- An Open-label Study in Healthy Participants to Evaluate AZD0780 as an Object or Precipitant of CYP3A4-mediated Drug-drug Interactions
In development for (1)
- Hyperlipidemia Phase 2