Tenapanor hydrochloride
Tenapanor hydrochloride Basic information
- Product Name:
- Tenapanor hydrochloride
- Synonyms:
-
- Tenapanor HCl
- Tenapanor dihydrochloride
- Tenapanor hydrochloride
- AZD-1722; AZD 1722; AZD1722; RDX 5791; RDX-5791; RDX5791; TENAPANOR; TENAPANOR HYDROCHLORIDE; TENAPANOR DIHYDROCHLORIDE; IBSRELA.
- 17-[[[3-[(4S)-6,8-Dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]-N-[2-[2-[2-[[[3-[(4S)-6,8-dichloro-1,2,3,4-tetrahydro-2-methyl-4-isoquinolinyl]phenyl]sulfonyl]amino]ethoxy]ethoxy]ethyl]-8-oxo-12,15-dioxa-2,7,9-triazaheptadecanamide dihydrochloride
- AZD1722 hydrochloride
- RDX5791 hydrochloride
- Tenapanor 2HCl
- CAS:
- 1234365-97-9
- MF:
- C50H68Cl6N8O10S2
- MW:
- 1217.97052
- EINECS:
- 810-634-7
- Mol File:
- 1234365-97-9.mol
Tenapanor hydrochloride Chemical Properties
- storage temp.
- -20°C
- solubility
- DMSO: soluble
- form
- A crystalline solid
- color
- White to off-white
- Water Solubility
- Water: soluble
- InChIKey
- VFRAXTZDILCRKY-OWRGXFNZSA-N
Tenapanor hydrochloride Usage And Synthesis
Uses
Tenapanor (AZD1722) HCl is a potent, orally active sodium/hydrogen exchanger isoform 3 (NHE3) inhibitor. Tenapanor HCl reduces intestinal phosphate absorption predominantly through the reduction of passive paracellular phosphate flux. Tenapanor HCl has the potential to be used in research on hyperphosphatemia.
Mechanism of action
Tenapanor hydrochloride is a minimally absorbed small molecule sodium/hydrogen exchange isomer 3 (NHE3) inhibitor. NHE3 is involved in the uptake of sodium ions and water into the intestinal lumen, and by inhibiting NHE3, tenapanor is expected to reduce sodium absorption and increase fecal sodium and fluid excretion.
Side effects
Tenapanor hydrochloride is generally well tolerated, with diarrhea being the most common adverse reaction. Diarrhea is usually transient (lasting 1 week) and mild to moderate in severity. Diarrhea develops within a week of starting treatment in approximately half of cases and within the first 3 weeks of treatment in two-thirds of cases. Other possible side effects include abdominal pain, nausea, bloating, and flatulence[1].
Synthesis
Synthesis of Tenapanor hydrochloride
in vivo
Tenapanor hydrochloride (0.15, 0.5 mg/kg; p.o.) reduces passive paracellular phosphate absorption in rats[1].
Tenapanor hydrochloride (0.15 mg/kg; p.o.; twice-daily for 11 consecutive days) increases the reduction in urinary phosphorus excretion in rats[2].
| Animal Model: | Rats (intestinal loop model)[1] |
| Dosage: | 0.15, 0.5 mg/kg |
| Administration: | P.o. |
| Result: | Reduced passive paracellular phosphate absorption by reduced urinary phosphate and sodium excretion after the high-phosphate meal and increased sodium and phosphate delivery to the cecum. |
| Animal Model: | 8 weeks, 250 g male Sprague–Dawley rats[2] |
| Dosage: | 0.15 mg/kg in combination with sevelamer (0%, 0.75%, 1.5%, and 3% (wt/wt)) |
| Administration: | Oral gavage; twice-daily for 11 consecutive days |
| Result: | Significantly augmented the reduction in urinary phosphorus excretion. |
References
[1] WILLIAM D CHEY. Efficacy of Tenapanor in Treating Patients With Irritable Bowel Syndrome With Constipation: A 26-Week, Placebo-Controlled Phase 3 Trial (T3MPO-2).[J]. American Journal of Gastroenterology, 2021, 116 6: 1294-1303. DOI:10.14309/ajg.0000000000001056.
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