Repositioning Candidate Details
| Candidate ID: | R1402 |
| Source ID: | DB11761 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Tenapanor |
| Synonyms: | Tenapanor |
| Molecular Formula: | C50H66Cl4N8O10S2 |
| SMILES: | CN1C[C@@H](C2=CC(=CC=C2)S(=O)(=O)NCCOCCOCCNC(=O)NCCCCNC(=O)NCCOCCOCCNS(=O)(=O)C2=CC(=CC=C2)[C@@H]2CN(C)CC3=C2C=C(Cl)C=C3Cl)C2=C(C1)C(Cl)=CC(Cl)=C2 |
| Structure: |
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| DrugBank Description: | Tenapanor is a novel, small molecule medication approved in September 2019 for the treatment of constipation-predominant irritable bowel-syndrome (IBS-C). It was first designed and synthesized in 2012. As an inhibitor of the sodium/hydrogen exchanger isoform 3 (NHE3) transporter, it is the first and currently only medication within its class and therefore exists as a novel alternative in the treatment of IBS-C. |
| CAS Number: | 1234423-95-0 |
| Molecular Weight: | 1145.04 |
| DrugBank Indication: | Tenapanor is indicated for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) in adults. It is also currently being investigated as a treatment for hyperphosphatemia in chronic kidney disease patients undergoing dialysis (NCT02081534 and NCT02675998). |
| DrugBank Pharmacology: | Through the inhibition of dietary sodium absorption tenapanor causes an increase in water secretion into the intestines, thereby decreasing transit time and softening stool consistency. |
| DrugBank MoA: | Tenapanor is a locally-acting small molecule inhibitor of the sodium/hydrogen exchanger isoform 3 (NHE3), an antiporter expressed on the apical surface of enterocytes in the small intestine and colon which is involved in sodium-fluid homeostasis. By inhibiting this antiporter tenapanor causes retention of sodium within the lumen of the intestine - this results in an osmotic gradient that draws water into the lumen and softens stool consistency. There is some evidence that tenapanor can inhibit the uptake of dietary phosphorus in the gastrointestinal tract, though the exact mechanism of this activity has yet to be elucidated. |
| Targets: | Sodium/hydrogen exchanger 3 inhibitor |
| Inclusion Criteria: | Indication associated |
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