Vericiguat

Highest phase reached
Approved
www.ebi.ac.uk
Drug type
Small molecule
www.ebi.ac.uk
First approval year
2021
www.ebi.ac.uk

First approval year
2021
www.ebi.ac.uk
Listing at source
Listed
Highest phase reached
Approved
www.ebi.ac.uk

Drug type
Small molecule
www.ebi.ac.uk
Drug name
Vericiguat
www.ebi.ac.uk
Molecular weight
426.39
www.ebi.ac.uk
Structure (SMILES)
COC(=O)Nc1c(N)nc(-c2nn(Cc3ccccc3F)c3ncc(F)cc23)nc1N
www.ebi.ac.uk

  • verquvo
  • Verquvo

  • bay 1021189
  • BAY 1021189
  • BAY-1021189
  • mk 1242
  • MK-1242
  • vericiguat
  • Vericiguat
  • vericiguat (BAY 1021189)
  • Vericiguat (BAY1021189)
  • Vericiguat (BAY1021189) (1.25 mg)
  • Vericiguat (BAY1021189) (5 mg)
  • Vericiguat (BAY1021189) 5 mg
  • Vericiguat [INN]
  • Vericiguat [JAN]
  • Vericiguat [MI]
  • Vericiguat [ORANGE BOOK]
  • Vericiguat [USAN]
  • Vericiguat [WHO-DD]
  • Vericiguat 10 MG
  • vericiguat inn
  • vericiguat jan
  • vericiguat mi
  • Vericiguat Oral Tablet
  • vericiguat orange book
  • Vericiguat suspension

And 3 more, listed on the interactive page.

CAS registry numbers
  • 1350653-20-1
ChEMBL ID
CHEMBL4066936
www.ebi.ac.uk
InChIKey
QZFHIXARHDBPBY-UHFFFAOYSA-N
www.ebi.ac.uk
PubChem compound IDs
  • 54674461
RxNorm IDs (RxCUI)
  • 2475830
FDA ingredient codes (UNII)
  • LV66ADM269

  • C01
  • C01DX22
Sources for recorded values
www.ebi.ac.uk

Applicant
MSD
Approval date
19 Jan 2021
Application number
NDA214377

Status
Authorised
Status date
16 Jul 2021
Authorisation date
16 Jul 2021
Approved indications
Treatment of symptomatic chronic heart failure
Product number
EMEA/H/C/005319
Authorisation holder
Bayer AG
Priority medicines scheme
No
Generic
No
Biosimilar
No
Generic medicines
0
Biosimilar medicines
0
Advanced therapy
No
Conditional approval
No
Additional monitoring
No
Accelerated assessment
No
Exceptional circumstances
No

Therapeutic areas

  • Heart Failure
European medicines record
www.ema.europa.eu

Patents
6
Designations
2
Earliest recorded loss of exclusivity
26 Nov 2032
First in class
Yes
Fast track
Yes
Breakthrough designation
No
Orphan designation
No
Priority review
Yes
Orphan exclusivity
No
Accelerated approval
No
Availability
Prescription only
Boxed warning
Yes

Pharmacology name
vericiguat
Type
Synthetic organic
Drug name stem
-ciguat
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • Oral

  • Action
    Activation
    Action type
    ACTIVATION
    Target
    Guanylyl cyclase, α2β1
    Gene symbol
    GUCY1A2
    Protein identifier
    P33402
  • Action
    Activation
    Action type
    ACTIVATION
    Target
    Guanylyl cyclase, α1β1
    Gene symbol
    GUCY1A1
    Protein identifier
    Q02108
  • Action
    Activation
    Action type
    ACTIVATION
    Target
    Guanylyl cyclase, α1β1
    Gene symbol
    GUCY1B1
    Protein identifier
    Q02153
  • Mechanism
    Soluble guanylate cyclase activator
    Action type
    ACTIVATOR
    Target
    Soluble guanylate cyclase
    Protein identifier
    O75343
  • Mechanism
    Soluble guanylate cyclase activator
    Action type
    ACTIVATOR
    Target
    Soluble guanylate cyclase
    Protein identifier
    P33402
  • Mechanism
    Soluble guanylate cyclase activator
    Action type
    ACTIVATOR
    Target
    Soluble guanylate cyclase
    Protein identifier
    Q02108
  • Mechanism
    Soluble guanylate cyclase activator
    Action type
    ACTIVATOR
    Target
    Soluble guanylate cyclase
    Protein identifier
    Q02153

Open Targets mechanisms

  • Mechanism
    Soluble guanylate cyclase activator
    Action type
    ACTIVATOR
    Target
    Soluble guanylate cyclase

DrugCentral mechanisms

  • Action type
    ACTIVATOR
    Gene symbol
    GUCY1B3
    Protein identifier
    Q02153
    Organism
    Homo sapiens
    Target development level
    Clinical

  • Condition
    Cardiovascular Diseases
    Highest recorded phase
    4
    Condition identifier
    EFO:0000319
    Subject identifier
    D002318
  • Condition
    Coronary Disease
    Highest recorded phase
    1
    Condition identifier
    EFO:0001645
    Subject identifier
    D003327
  • Condition
    Heart Failure
    Highest recorded phase
    4
    Condition identifier
    EFO:0003144
    Subject identifier
    D006333

  • Condition identifier
    EFO_0000319
  • Condition identifier
    EFO_0001645
    Highest recorded phase
    1
  • Condition identifier
    EFO_0003144
  • Condition identifier
    HP_0000855
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0004995
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0005010
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005252
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0005356
    Highest recorded phase
    2

Warnings

  • Warning
    Black Box Warning
    Effect
    teratogenicity

Open Targets warnings

  • Warning
    Black Box Warning
    Effect
    teratogenicity
    Country
    United States

Reported adverse events

  • Event
    cardiac failure
    Reports
    4
    Reporting signal score
    12.8117

Dose
2.5-5mg
Route
Oral
How often
Once daily

Conditions of use

  • Take with food

Hydrogen bond acceptors
9
Hydrogen bond donors
3
Polar surface area
146.86
Calculated partition coefficient (ALogP)
2.56
Calculated partition coefficient (XLogP)
1.5
Prodrug
No
Chirality
Achiral
Inorganic
No
Rule-of-five violations
0
Rotatable bonds
4
Heavy atoms
31
Molecular formula
C19H16F2N8O2
Monoisotopic mass
426.13642811
Natural product
No

  • 0006-5028
  • 0006-5029
  • 0006-5030

Recorded assays
51
Active assays
11

Active assay types

  • Confirmatory

Oral bioavailability

Median
70
Mean
70
Minimum
65
Maximum
75
Unit
%
Assays
2
Standard deviation
7.07107
Summary method
median
Censored results excluded
0
Other units excluded
0
Unknown units excluded
0

Measurement types

  • F

Related records

Trials (43)

Approved for (2)

In development for (1)

Targets (4)