phenformin
Phenformin is a biguanide hypoglycemic agent with actions and uses similar to those of metformin. It activates AMP-activated protein kinase (AMPK) and inhibits mTORC1 signaling. Phenformin used for the treatment of diabetes. Phenformin was removed from the U.S. market 20 years ago because of a high incidence of lactic acidosis. Risk factors for the development of lactic acidosis include renal deficiency, hepatic disease, cardiac disease, and drug interaction such as cimetidine. Phenformin exerts potential anti-neoplastic action. — NCATS
Clinical trial activity
2 trials · 5 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 2017 (NCT03026517)
Timeline
2010s
- Jan 1, 2017
Earliest Phase 1 Sponsor(trial)
Indications
Approved for
Studied for
Mechanism of action
- Unspecified targetOTHER
Unknown
Inhibitor of Complex I of the mitochondrial respiratory chain. It activates AMP-activated protein kinase (AMPK).The mechanism of activation remains uncertain.
Chemistry & pharmacology
SMILES
N=C(N)NC(=N)NCCc1ccccc1- Mol. weight
- 205.26 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL170988 ↗
- WikipediaPhenformin ↗
- NCATS91XC93EU03 ↗
- ChEMBLCHEMBL1528839 ↗
Also known as
- 5-methoxy-2-methyl-3-indoleacetic acid
- 5-methoxy-methylindoleacetic acid
- dbi
- dbi
- dbi
- dbi
- (des-4-chlorobenzoyl)indomethacin
- deschlorobenzoylindomethacin
- dibotin s.r.
- fenformin
- fenformin
- fenformina
- fenformina
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformin
- phenformine
- phenformine
- phenformin hcl
- phenformin hcl
- phenformin hcl
- phenformin hydrochloride
- phenformin hydrochloride
- phenformin hydrochloride
- phenforminum
- phenforminum
- β-phenethybiguanide
- β-phenethybiguanide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05003492 | Phase 1/Phase 2 (Phase 2) | Sep 30, 2021 | Damitta University, Government of Saudi Arabia, Kafrelsheikh University |
| NCT03026517 | Phase 1 | Jan 1, 2017 | Cornell University, Harvard University |
Organizations
Research & Development (5)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cornell University | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Damitta University | Academic/Hospital | 1 | 0 | 1 | 2021 |
| Government of Saudi Arabia | Government | 1 | 1 | 1 | 2021 |
| Harvard University | Academic/Hospital | 1 | 0 | 1 | 2017 |
| Kafrelsheikh University | Academic/Hospital | 1 | 0 | 1 | 2021 |