istradefylline
Trade name: Nourianz
Small moleculeapproved
Approved
Aug 27, 2019
Istradefylline is a first-in-class adenosine A2A receptor antagonist antiparkinsonian agent and has been marketed as the brand name NOURIAST® in Japan since May 30, 2013. NOURIAST is indicated for the improvement of wearing-off phenomena in patients with Parkinson’s disease on concomitant treatment with levodopa-containing products. — NCATS
Clinical trial activity
26 trials · 9 clinical orgs · 1 marketing orgs
Phase 1
5
Phase 2
21
Phase 3
11
Phase 4
1
Earliest trial started Oct 1, 2000 (NCT00006337)
Timeline
2010s
- Jan 1, 2014
Earliest Phase 1 Sponsor(trial)
- Aug 27, 2019
Kyowa Kirin — Earliest FDA Approval
- Aug 27, 2019
Kyowa Kirin — Marketing Organization
- Aug 27, 2019
Kyowa Kirin — NDA Organization
Indications
Approved for
Studied for
- Amyotrophic Lateral Sclerosis · Phase 1/Phase 2
- Cognitive Dysfunction · Phase 2
- Liver Diseases · Phase 1
- Movement Disorders · Phase 2
- Parkinson Disease · Phase 4
- Restless Legs Syndrome · Phase 2
- Sleep Wake Disorders · Phase 2
- Spinal Cord Diseases · Phase 1/Phase 2
- Spinal Cord Injuries · Phase 1/Phase 2
- Substance-Related Disorders · Phase 1
- Tremor · Phase 4
Mechanism of action
- Adenosine A2a receptorANTAGONIST
ADORA2A antagonist
Approval history
- approvedAug 27, 2019
Chemistry & pharmacology
Loading structure…
SMILES
CCN1C2=C(N(C)C(\C=C\C3=CC(OC)=C(OC)C=C3)=N2)C(=O)N(CC)C1=O- Mol. weight
- 384.429 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
First in class
Sources
- WikipediaIstradefylline ↗
- NCATS2GZ0LIK7T4 ↗
- ChEMBLCHEMBL431770 ↗
Also known as
- 8-(2-(3,4-dimethoxyphenyl)ethenyl)-1,3-diethyl-3,7-dihydro-7-methyl-1h-purine-2,6-dione
- istradefylline
- istradefylline
- istradefylline
- istradefylline
- istradefylline
- istradefylline
- istradefylline
- istradefylline
- kw6002
- kw 6002
- kw-6002
- kw-6002
- kw-6002
- kw-6002
- kw-6002
- nouriast
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05885360 | Phase 4 | Jan 20, 2023 | Georgetown University, Kyowa Hakko Kirin |
| NCT05217498 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2022 | Harvard University |
| NCT05333549 | Phase 2 | Jul 18, 2022 | Kyowa Hakko Kirin, Virginia Commonwealth University |
| NCT05377424 | Phase 1/Phase 2 (Phase 2) | Jun 21, 2022 | ALS Association, University of Florida |
| NCT02609477 | Phase 1 | Jan 1, 2016 | Kyowa Hakko Kirin |
| NCT02610231 | Phase 3 | Dec 1, 2015 | Kyowa Hakko Kirin |
| NCT02256033 | Phase 1 | Aug 1, 2014 | Kyowa Hakko Kirin |
| NCT02174250 | Phase 1 | Jun 1, 2014 | Kyowa Hakko Kirin |
| NCT01968031 | Phase 3 | Oct 1, 2013 | Kyowa Hakko Kirin |
| NCT00957203 | Phase 3 | Oct 1, 2009 | Kyowa Hakko Kirin |
| NCT00955526 | Phase 3 | Jul 1, 2009 | Kyowa Hakko Kirin |
| NCT00455507 | Phase 2 | Mar 1, 2007 | Kyowa Hakko Kirin |
| NCT00250393 | Phase 2 | Nov 1, 2005 | Kyowa Hakko Kirin |
| NCT00199381 | Phase 3 | Oct 1, 2005 | Kyowa Hakko Kirin, Kyowa Kirin |
| NCT00199446 | Phase 2 | Jul 1, 2005 | Kyowa Hakko Kirin, Kyowa Kirin |
| NCT00199433 | Phase 2 | May 1, 2005 | Kyowa Hakko Kirin, Kyowa Kirin |
| NCT00199355 | Phase 2 | Apr 1, 2005 | Kyowa Hakko Kirin |
| NCT00203957 | Phase 3 | Mar 1, 2005 | University of Chicago |
| NCT00199394 | Phase 3 | Nov 1, 2004 | Kyowa Hakko Kirin |
| NCT00199368 | Phase 3 | Oct 1, 2004 | Kyowa Hakko Kirin, Kyowa Kirin |
Showing 20 of 26 trials
Page 1 / 2
Organizations
Research & Development (9)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Kyowa Hakko Kirin | For profit | 22 | 20 | 4 | 2002 |
| Kyowa Kirin | For profit | 8 | 0 | 2 | 2002 |
| ALS Association | Academic/Hospital | 1 | 0 | 1 | 2022 |
| Georgetown University | Academic/Hospital | 1 | 1 | 1 | 2023 |
| Harvard University | Academic/Hospital | 1 | 1 | 1 | 2022 |
| National Institute of Neurological Disorders and Stroke (NINDS) | Government | 1 | 1 | 1 | 2000 |
| University of Chicago | Academic/Hospital | 1 | 1 | 1 | 2005 |
| University of Florida | Academic/Hospital | 1 | 1 | 1 | 2022 |
| Virginia Commonwealth University | Academic/Hospital | 1 | 1 | 1 | 2022 |
9 organizations
Page 1 / 1
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Kyowa Kirin | For profit | MKTG | Aug 27, 2019 |
| Kyowa Kirin | For profit | NDA | Aug 27, 2019 |