UCSF home page About UCSF UCSF Medical Center
UCSF home page | About UCSF | UCSF Medical Center

Skip to TransPortal content

Decrease the text sizeRestore original text sizeIncrease the text size Enlarge Text
Click to increase the text size.
Restore Text
Click to restore original text size.
Reduce Text
Click to decrease the text size.
Transporter Database banner  
Decrease the text size | Restore text size | Increase the text size
Text Sizer image
Home About and More Information Transporter Data Index
Search:  
 

Pyrimethamine

Substrate Information
Inhibitor Information
Clinical Drug-drug Interactions

In Vitro Substrates

No substrate information.


Back to top

In Vitro Inhibitors

* denotes drugs that can potentially be used for in vivo (clinical) studies of the designated transporter
Transporter Synonyms Inhibitor IC50 (μM) Ki (μM) Substrate used Cell System Reference
SLC47A2 MATE2K Pyrimethamine 0.059 1-methyl-4-phenylpyridinium (MPP+) CHO-MATE2K Astorga, 2012
SLC22A2 OCT2 Pyrimethamine 23.6 1-methyl-4-phenylpyridinium (MPP+) HEK293-OCT2 Shen, 2013
SLC22A1 OCT1 Pyrimethamine 8.5 1-methyl-4-phenylpyridinium (MPP+) MDCK-OCT1 Hubeny, 2016
SLC22A1 OCT1 Pyrimethamine 13.57 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT1 Chen, 2017
SLC22A2 OCT2 Pyrimethamine 1.6 4-(4-dimethylamino)styryl-N-methylpyridinium (ASP+) HEK293-OCT2 van, 2017
SLC47A1 MATE1 Pyrimethamine 0.07 Ipratropium HEK293-MATE1 Chen, 2017
SLC47A2 MATE2K Pyrimethamine 0.01 Ipratropium HEK293-MATE2K Chen, 2017
SLC22A2 OCT2 Pyrimethamine 4.8 Metformin HEK293-OCT2 Shen, 2013
SLC22A1 OCT1 Pyrimethamine 4.46 Metformin Caco-OCT1 Elsby, 2017

Back to top

Clinical Drug-Drug Interactions

DDI Implicated Transporter* Interacting Drug Affected Drug AUC Cmax CLR CL/F t1/2 Effect on PD Reference More Details
Clinical PK Impact(fold change)
1 MATEs Pyrimethamine Metformin 1.4 1.4 0.6 ND ND ND Kusuhara, 2011 DDI 1

PK = pharmacokinetic
The transporters are implicated by in vitro data and/or studies in humans with genetic polymorphisms of the transporter
DDI = Drug Drug Interaction
PD = pharmacodynamic
ND = not determined
NS = not significant
N/A = information not available
Calculation of Fold Change: fold change in the presence of the interacting drug = (value with interacting drug)/(value without interacting drug)
fold change > 1: increase in pharmacokinetic value
fold change < 1: decrease in pharmacokinetic value


Back to top

Contact us | Glossary

Blue banner