Alosetron Hydrochloride

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Cat Number

API0231947

CAS Number

122852-69-1

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Product Detail Description Scientific Support Customer Q&A

CAS Number

122852-69-1

EINECS

802-450-0

Storage

Store at room temperature

Synonyms

Alosetron HCl; GR 68755c; Lotrpnex; DTXSID8044208; GR-68755C; 2F5R1A46YW; DTXCID6024208

Molecular Formula

C17H19ClN4O

Molecular Weight

330.8

Smiles

CC1=C(N=CN1)CN2CCC3=C(C2=O)C4=CC=CC=C4N3C.Cl

Appearance

White to off-white crystalline powder

Melting Point

288-291°C

Boiling Point

648.1°C at 760 mmHg

Relative Density

1.34

General Description

Alosetron hydrochloride is a synthetic imidazole derivative, a potent and selective serotonin 5-HT3 receptor antagonist. Its chemical structure is 2,3,4,5-tetrahydro-5-methyl-1H-pyrido[4,3-b]indol-1-one hydrochloride. Alosetron is a white to off-white crystalline powder that is freely soluble in water.

Mechanism of Action

Alosetron acts as a highly selective antagonist at 5-HT3 receptors, which are located predominantly in the gastrointestinal tract, particularly on enteric neurons and the central nervous system. By blocking these receptors, it reduces the release of serotonin and other neurotransmitters, slowing colonic transit and decreasing visceral hypersensitivity.

Application

Alosetron is indicated for the treatment of severe, chronic diarrhea-predominant irritable bowel syndrome (IBS) in women who have failed to respond to conventional therapy.

This 12‑week prospective open‑label study evaluated alosetron in 192 women with severe IBS‑D using rigorous FDA‑mandated composite endpoints. The most common dosing was 0.5 mg twice daily. Among 105 fully evaluable patients, 45% met the composite responder criteria (≥30% reduction in worst abdominal pain and ≥50% reduction in days with type 6/7 stools) for ≥50% of the study period. All individual symptom domains, including fecal urgency and incontinence, improved significantly. No serious adverse events, colonic ischemia, or constipation complications occurred. Alosetron demonstrated efficacy and safety in clinical practice.

Fig. 1 Efficacy of alosetron in women with severe irritable-bowel-syndrome-associated diarrhea. (Lacy BE, et al., 2018)

References

Lacy BE, et al. Alosetron use in clinical practice: significant improvement in irritable bowel syndrome symptoms evaluated using the US Food and Drug Administration composite endpoint. Ther Adv Gastroenterol. 2018;11:1756284818771674.

Does Alosetron Hydrochloride require protection from light during long-term storage?

Yes, it is photosensitive. UV exposure can cause photodegradation of the imidazole ring. Store in light-resistant containers, preferably amber glass.

What is the recommended storage temperature for Alosetron Hydrochloride?

Store at controlled room temperature (15–25°C). Avoid excessive heat above 30°C, which can soften the powder and accelerate oxidation.

Is Alosetron Hydrochloride stable in tablet formulations with standard excipients?

Yes, when formulated with moisture-protective packaging.

How is the impurity alosetron N-oxide (an oxidative degradation product) monitored?

This degradation product is quantified using a stability-indicating HPLC method, ensuring it remains within ICH qualification thresholds.