> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/rizatriptan-62bc4777-817b-40f6-b936-bbc1eba350d2
> Record changed: 2026-10-13

# Rizatriptan

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

First approval year

1998

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

## Development status

**First approval year**

1998

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**Drug name**

Rizatriptan

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**Molecular weight**

269.35

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**Structure (SMILES)**

CN(C)CCc1c\[nH\]c2ccc(Cn3cncn3)cc12

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

### Brand names (2)

- maxalt
- Maxalt

### Other names (14)

- 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

## Identifiers

**ATC classification codes**

- N02CC04

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**CAS registry numbers**

- 144034-80-0

**ChEMBL ID**

CHEMBL905

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**InChIKey**

ULFRLSNUDGIQQP-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL905)

**PubChem compound IDs**

- 5078

**FDA ingredient codes (UNII)**

- 51086HBW8G

### RxNorm IDs (RxCUI) (2)

- 88014
- 237082

## Regulatory information

### United States

**Applicant**

ORGANON LLC

**Approval date**

29 Jun 1998

**Application number**

NDA020864

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

**Boxed warning**

Yes

## Pharmacology

### Drug classification

**Pharmacology name**

rizatriptan

**Type**

Synthetic organic

**Drug name stem**

\-triptan

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (5)

- **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

### Open Targets mechanisms (2)

- **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

### DrugCentral mechanisms (4)

- **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

### Investigated indications (3)

- **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

### Open Targets indications (6)

- **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

### Reported adverse events (74)

- **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

And 49 more, listed on the interactive page.

### Trial references (15)

- NCT00246337  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00246337)
- NCT00250458  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00250458)
- NCT00300924  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00300924)
- NCT00397254  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00397254)
- NCT00443209  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00443209)
- NCT00753311  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00753311)
- NCT00894556  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00894556)
- NCT01001234  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01001234)
- NCT01057160  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01057160)
- NCT01286207  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01286207)
- NCT03896009  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03896009)
- NCT04163185  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04163185)
- NCT04384367  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04384367)
- NCT05550207  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05550207)
- NCT00471952  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00471952)

## Dosing

**Dose**

5-10mg

**Route**

Oral

**How often**

As needed, up to 4 doses in 24 hours

### Conditions of use (2)

- Do not prescribe to pediatric patients <40kg on propranolol
- Max 30mg per 24 hours

## Chemical properties

**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

## Evidence counts

**Recorded assays**

642

**Active assays**

65

### Active assay types (2)

- Confirmatory
- Other

## Pharmacologic actions

- Serotonin Receptor Agonists  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D017366.html)

## Biological measurements

### Observed measurements

#### 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](https://trialight.com/data/trial/efficacy-and-safety-of-rizatriptan-naproxen-10-550-mg-in-the-70efddef-4813-48a4-864f-4182d7fde312.md)
- 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)

- [Migraine disorder](https://trialight.com/data/condition/migraine-disorder-0a28e77d-6415-5582-980f-2d0721f95f76.md)

### In development for (2)

- [Migraine with aura](https://trialight.com/data/condition/migraine-with-aura-e2c8f3b7-7f7f-5f92-9eee-1fe843c3d45b.md) Phase 3
- [Migraine without aura](https://trialight.com/data/condition/migraine-without-aura-107a1c43-76b2-5352-b954-9838b0891157.md) Phase 3

### Targets (2)

- [HTR1B](https://trialight.com/data/target/htr1b-f109dd33-597e-57af-8498-727af113b42b.md) Serotonin 1b (5-HT1b) receptor agonist
- [HTR1D](https://trialight.com/data/target/htr1d-8c6c6eaa-650d-574b-b5ed-aa796d90ad80.md) Serotonin 1d (5-HT1d) receptor agonist

---

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