Rizatriptan
Highest phase reached
Approved
Drug type
Small molecule
First approval year
1998
- First approval year
- 1998
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Rizatriptan
- Molecular weight
- 269.35
- Structure (SMILES)
- CN(C)CCc1c[nH]c2ccc(Cn3cncn3)cc12
- maxalt
- Maxalt
- l 705126
- L-705126
- mk 462 free base
- MK-462 FREE BASE
- rizatriptan
- Rizatriptan
- rizatriptan [INN]
- RIZATRIPTAN [MI]
- RIZATRIPTAN [VANDF]
- Rizatriptan [WHO-DD]
- rizatriptan inn
- rizatriptan mi
- rizatriptan vandf
- rizatriptan who dd
- ATC classification codes
- N02CC04
Sources for recorded values
- CAS registry numbers
- 144034-80-0
- ChEMBL ID
- CHEMBL905
- InChIKey
- ULFRLSNUDGIQQP-UHFFFAOYSA-N
- PubChem compound IDs
- 5078
- FDA ingredient codes (UNII)
- 51086HBW8G
- 88014
- 237082
- Applicant
- ORGANON LLC
- Approval date
- 29 Jun 1998
- Application number
- NDA020864
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- Boxed warning
- Yes
- Pharmacology name
- rizatriptan
- Type
- Synthetic organic
- Drug name stem
- -triptan
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- 5-HT1A receptor
- Gene symbol
- HTR1A
- Protein identifier
- P08908
- Median affinity
- 6.4
- Affinity units
- pKi
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- 5-HT1D receptor
- Gene symbol
- HTR1D
- Protein identifier
- P28221
- Median affinity
- 7.9
- Affinity units
- pKi
- Primary target
- Yes
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- 5-ht1e receptor
- Gene symbol
- HTR1E
- Protein identifier
- P28566
- Median affinity
- 6.8
- Affinity units
- pKi
- Action
- Full agonist
- Action type
- FULL_AGONIST
- Target
- 5-HT1F receptor
- Gene symbol
- HTR1F
- Protein identifier
- P30939
- Affinity units
- pKi
- Action
- Partial agonist
- Action type
- PARTIAL_AGONIST
- Target
- 5-HT1B receptor
- Gene symbol
- HTR1B
- Protein identifier
- P28222
- Median affinity
- 6.9
- Affinity units
- pKi
- Primary target
- Yes
- Mechanism
- Serotonin 1b (5-HT1b) receptor agonist
- Action type
- Agonist
- Target
- 5-hydroxytryptamine receptor 1B
- Mechanism
- Serotonin 1d (5-HT1d) receptor agonist
- Action type
- Agonist
- Target
- 5-hydroxytryptamine receptor 1D
- Action type
- Agonist
- Gene symbol
- HTR1D
- Protein identifier
- P28221
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- HTR1B
- Protein identifier
- P28222
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Agonist
- Gene symbol
- HTR1E
- Protein identifier
- P28566
- Organism
- Homo sapiens
- Target development level
- Chemical evidence
- Action type
- Agonist
- Gene symbol
- HTR1F
- Protein identifier
- P30939
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Migraine Disorders
- Highest recorded phase
- 4
- Condition identifier
- MONDO:0005277
- Subject identifier
- D008881
- Condition
- Migraine with Aura
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0005475
- Subject identifier
- D020325
- Condition
- Migraine without Aura
- Highest recorded phase
- 3
- Condition identifier
- MONDO:0100431
- Subject identifier
- D020326
- Condition identifier
- EFO_0006928
- Condition identifier
- HP_0002321
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005277
- Condition identifier
- MONDO_0005277
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005475
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0100431
- Highest recorded phase
- 3
Open Targets warnings
- Warning
- Black Box Warning
- Country
- United States
- Event
- abdominal pain
- Reports
- 36
- Reporting signal score
- 15.4144
- Event
- abdominal pain upper
- Reports
- 25
- Reporting signal score
- 12.8792
- Event
- acute respiratory failure
- Reports
- 12
- Reporting signal score
- 21.3804
- Event
- alanine aminotransferase increased
- Reports
- 22
- Reporting signal score
- 16.1219
- Event
- anuria
- Reports
- 13
- Reporting signal score
- 29.1757
- Event
- arteriospasm coronary
- Reports
- 6
- Reporting signal score
- 12.0329
- Event
- aspartate aminotransferase increased
- Reports
- 21
- Reporting signal score
- 16.5647
- Event
- atheroembolism
- Reports
- 3
- Reporting signal score
- 13.7456
- Event
- blood chloride decreased
- Reports
- 6
- Reporting signal score
- 14.3818
- Event
- blue toe syndrome
- Reports
- 3
- Reporting signal score
- 11.7439
- Event
- broad ligament tear
- Reports
- 3
- Reporting signal score
- 22.2346
- Event
- carotid artery dissection
- Reports
- 7
- Reporting signal score
- 30.1359
- Event
- chest discomfort
- Reports
- 26
- Reporting signal score
- 22.9962
- Event
- chest pain
- Reports
- 31
- Reporting signal score
- 16.5943
- Event
- colitis ischaemic
- Reports
- 27
- Reporting signal score
- 83.8407
- Event
- coronary artery dissection
- Reports
- 10
- Reporting signal score
- 41.0642
- Event
- cough
- Reports
- 38
- Reporting signal score
- 18.9513
- Event
- drug abuse
- Reports
- 27
- Reporting signal score
- 32.2254
- Event
- drug hypersensitivity
- Reports
- 46
- Reporting signal score
- 23.0021
- Event
- drug interaction
- Reports
- 45
- Reporting signal score
- 29.0101
- Event
- duodenal ulcer
- Reports
- 8
- Reporting signal score
- 13.4789
- Event
- dust allergy
- Reports
- 3
- Reporting signal score
- 11.6557
- Event
- dyspepsia
- Reports
- 16
- Reporting signal score
- 12.7628
- Event
- extrapyramidal disorder
- Reports
- 13
- Reporting signal score
- 20.7097
- Event
- gallbladder polyp
- Reports
- 14
- Reporting signal score
- 67.1793
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- Dose
- 5-10mg
- Route
- Oral
- How often
- As needed, up to 4 doses in 24 hours
- Do not prescribe to pediatric patients <40kg on propranolol
- Max 30mg per 24 hours
- Hydrogen bond acceptors
- 4
- Hydrogen bond donors
- 1
- Polar surface area
- 49.74
- Calculated partition coefficient (ALogP)
- 1.91
- Calculated partition coefficient (XLogP)
- 1.7
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 0
- Rotatable bonds
- 5
- Heavy atoms
- 20
- Molecular formula
- C15H19N5
- Monoisotopic mass
- 269.16404563
- Natural product
- Yes
- Recorded assays
- 642
- Active assays
- 65
- Confirmatory
- Other
- Serotonin Receptor Agonists
Distribution coefficient (LogD)
- Median
- -0.74
- Mean
- -0.74
- Minimum
- -0.74
- Maximum
- -0.74
- Unit
- unitless
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- LogD
Oral bioavailability
- Median
- 45
- Mean
- 45
- Minimum
- 45
- Maximum
- 45
- Unit
- %
- Assays
- 1
- Standard deviation
- 0
- Summary method
- median
- Censored results excluded
- 0
- Other units excluded
- 0
- Unknown units excluded
- 0
Measurement types
- F
Related records
Trials (15)
- A Dose-Finding Study of MK0974 in Acute Migraine (MK0974-004)
- A Study of Rizatriptan Co-Administered With Acetaminophen for the Treatment of Acute Migraine
- A Study to Evaluate the Efficacy and Tolerability of Rizatriptan for Treatment of Acute Migraine (0462-087)
- A Study to Evaluate the Efficacy and Tolerability of Rizatriptan for Treatment of Acute Migraine in Children and Adolescents (MK-0462-082 AM7)
- Does a Migraine Medication Decrease Rotational Motion Sickness in People Suffering From Migraines?
- Efficacy and Safety of Rizatriptan-Naproxen (10/550 Mg) in the Acute Treatment of Migraine
- Initiating Early Control of Migraine Pain and Associated Symptoms
- Long-Term Exposure to Rizatriptan 5-mg and 10-mg Oral Tablet (Combined Extension Protocols MK-0462-022, MK-0462-025, MK-0462-029)
- Maximizing Outcomes in Treating Acute Migraine
- Rizatriptan 10 MG RPD in the Treatment of Acute Migraine
- Rizatriptan for Episodic Dizziness in Vestibular Migraine
- Study of Rizatriptan in the Treatment of Acute Attacks of Post-traumatic Headache in U.S. Military Troops
- Telcagepant (MK-0974) Long-Term Safety Study in Adult Participants With Acute Migraine (MK-0974-012)
- The Effects of Expectation and Knowledge on Rizatriptan and Placebo Treatment of Acute Migraine Headache
- Two Rizatriptan Prescribing Portions for Treatment of Migraine
Approved for (1)
In development for (2)
- Migraine with aura Phase 3
- Migraine without aura Phase 3