Rimegepant

Highest phase reached
Drug type
Small molecule
First approval year

First approval year
Listing at source
Listed
Highest phase reached

Drug type
Small molecule
Drug name
Rimegepant
Molecular weight
Structure (SMILES)
N[C@@H]1c2cccnc2[C@H](OC(=O)N2CCC(n3c(=O)[nH]c4ncccc43)CC2)CC[C@H]1c1cccc(F)c1F

  • bhv 3000
  • Bhv-3000
  • bms 927711
  • bms 927711 cgrp antagonist
  • BMS-927711
  • BMS-927711 (CGRP Antagonist)
  • rimegepant
  • Rimegepant
  • Rimegepant [INN]
  • Rimegepant [MI]
  • Rimegepant [USAN]
  • Rimegepant [WHO-DD]
  • rimegepant inn
  • rimegepant mi
  • rimegepant usan
  • rimegepant who dd

ATC classification codes
  • N02CD06
Sources for recorded values
CAS registry numbers
  • 1289023-67-1
ChEMBL ID
CHEMBL2178422
InChIKey
KRNAOFGYEFKHPB-ANJVHQHFSA-N
PubChem compound IDs
  • 51049968
RxNorm IDs (RxCUI)
  • 2282307
FDA ingredient codes (UNII)
  • 997WVV895X

Applicant
PFIZER
Approval date
27 Feb 2020
Application number
NDA212728

Status
Authorised
Status date
25 Apr 2022
Authorisation date
25 Apr 2022
Approved indications
Vydura is indicated for the Acute treatment of migraine with or without aura in adults; Preventative treatment of episodic migraine in adults who have at least 4 migraine attacks per month.
Product number
EMEA/H/C/005725
Authorisation holder
Pfizer Europe MA EEIG
Priority medicines scheme
No
Generic
No
Biosimilar
No
Generic medicines
0
Biosimilar medicines
0
Advanced therapy
No
Conditional approval
No
Additional monitoring
Yes
Accelerated assessment
No
Exceptional circumstances
No

Therapeutic areas

  • Migraine Disorders
European medicines record

First in class
No
Orphan designation
No
Availability
Prescription only

United States (FDA)
Approved
European Union (EMA)
Authorised

Pharmacology name
rimegepant
Type
Synthetic organic
Drug name stem
-gepant
Approval recorded by Guide to Pharmacology
Yes

Administration routes

  • Oral

  • Action
    Antagonist
    Action type
    Antagonist
    Target
    AMY1 receptor
    Gene symbol
    RAMP1
    Protein identifier
    O60894
    Median affinity
    8.1
    Affinity units
    pKB
  • Action
    Antagonist
    Action type
    Antagonist
    Target
    CGRP receptor
    Gene symbol
    RAMP1
    Protein identifier
    O60894
    Median affinity
    9.6
    Affinity units
    pKB
    Primary target
    Yes
  • Action
    Antagonist
    Action type
    Antagonist
    Target
    AMY1 receptor
    Gene symbol
    CALCR
    Protein identifier
    P30988
    Median affinity
    8.1
    Affinity units
    pKB
  • Action
    Antagonist
    Action type
    Antagonist
    Target
    CGRP receptor
    Gene symbol
    CALCRL
    Protein identifier
    Q16602
    Median affinity
    9.6
    Affinity units
    pKB
    Primary target
    Yes
  • Mechanism
    Calcitonin gene-related peptide type 1 receptor antagonist
    Action type
    Antagonist
    Target
    Calcitonin gene-related peptide type 1 receptor
    Protein identifier
    Q16602

Open Targets mechanisms

  • Mechanism
    Calcitonin gene-related peptide type 1 receptor antagonist
    Action type
    Antagonist
    Target
    Calcitonin gene-related peptide type 1 receptor

DrugCentral mechanisms

  • Action type
    Antagonist
    Gene symbol
    CALCRL
    Protein identifier
    Q16602
    Organism
    Homo sapiens
    Target development level
    Clinical

  • Condition
    Irritable Bowel Syndrome
    Highest recorded phase
    2
    Condition identifier
    EFO:0000555
    Subject identifier
    D043183
  • Condition
    Psoriasis
    Highest recorded phase
    2
    Condition identifier
    EFO:0000676
    Subject identifier
    D011565
  • Condition
    Pain
    Highest recorded phase
    2
    Condition identifier
    EFO:0003843
    Subject identifier
    D010146
  • Condition
    Temporomandibular Joint Disorders
    Highest recorded phase
    3
    Condition identifier
    EFO:0005279
    Subject identifier
    D013705
  • Condition
    Sinusitis
    Highest recorded phase
    3
    Condition identifier
    EFO:0007486
    Subject identifier
    D012852
  • Condition
    Trigeminal Neuralgia
    Highest recorded phase
    2
    Condition identifier
    EFO:1001219
    Subject identifier
    D014277
  • Condition
    Migraine Disorders
    Highest recorded phase
    3
    Condition identifier
    MONDO:0005277
    Subject identifier
    D008881

  • Condition identifier
    EFO_0000555
    Highest recorded phase
    2
  • Condition identifier
    EFO_0000676
    Highest recorded phase
    2
  • Condition identifier
    EFO_0005279
    Highest recorded phase
    3
  • Condition identifier
    EFO_0007486
    Highest recorded phase
    3
  • Condition identifier
    EFO_0008008
  • Condition identifier
    EFO_1001219
    Highest recorded phase
    2
  • Condition identifier
    HP_0002027
    Highest recorded phase
    2
  • Condition identifier
    HP_0012531
    Highest recorded phase
    2
  • Condition identifier
    HP_0100582
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0005052
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0005184
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0005277
  • Condition identifier
    MONDO_0005277
    Highest recorded phase
    4
  • Condition identifier
    MONDO_0005575
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0006031
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0006314
    Highest recorded phase
    3
  • Condition identifier
    MONDO_0008599
    Highest recorded phase
    2
  • Condition identifier
    MONDO_0009831
    Highest recorded phase
    1
  • Condition identifier
    MONDO_0021040
    Highest recorded phase
    1

  • Event
    decreased embryo viability
    Reports
    1
    Reporting signal score
    11.3267
  • Event
    drug interaction
    Reports
    3
    Reporting signal score
    9.57925

Dose
75 mg
Route
Oral
How often
As needed; every other day

Conditions of use

  • Take with or without food

Hydrogen bond acceptors
7
Hydrogen bond donors
2
Polar surface area
119.13
Calculated partition coefficient (ALogP)
4.49
Calculated partition coefficient (XLogP)
2.3
Prodrug
No
Chirality
Single enantiomer
Inorganic
No
Rule-of-five violations
1
Rotatable bonds
3
Heavy atoms
39
Molecular formula
C28H28F2N6O3
Monoisotopic mass
534.21909510
Natural product
No

Recorded assays
1,171
Active assays
7

Active assay types

  • Confirmatory

These details could not be displayed.

Related records

Trials (61)

In development for (12)

Targets (3)