Iloperidone

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Cat Number

API133454474

CAS Number

133454-47-4

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Product Detail Description Scientific Support Customer Q&A

CAS Number

133454-47-4

EINECS

603-745-5

Storage

Store at room temperature

Synonyms

Fanapt; Zomaril; HP-873; iloperidona; DTXSID6049060; VPO7KJ050N

Molecular Formula

C24H27FN2O4

Molecular Weight

426.5

Smiles

CC(=O)C1=CC(=C(C=C1)OCCCN2CCC(CC2)C3=NOC4=C3C=CC(=C4)F)OC

Appearance

White to almost white powder to crystal

Melting Point

122.0-126.0°C

Boiling Point

593.7±50.0°C at 760 mmHg

Relative Density

1.2±0.1

General Description

Iloperidone is a synthetic piperidine derivative with a benzisoxazole group, belonging to the class of atypical antipsychotics. Its chemical structure is 1-[4-[3-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]propoxy]-3-methoxyphenyl]ethanone. Iloperidone is a white to off-white powder, practically insoluble in water. It is a potent antagonist of dopamine D2 and serotonin 5-HT2A receptors.

Mechanism of Action

Iloperidone acts as a full antagonist at dopamine D2 receptors, which reduces the positive symptoms of schizophrenia, and as a potent antagonist at serotonin 5-HT2A receptors, which reduces the negative symptoms and extrapyramidal side effects. It also has weak affinity for alpha-1 adrenergic, histamine H1, and muscarinic receptors, contributing to its side effect profile.

Application

Iloperidone is indicated for the treatment of schizophrenia in adults. It is effective in reducing both positive and negative symptoms of the disease. The drug has a lower incidence of extrapyramidal side effects compared to first-generation antipsychotics, but it is associated with QT prolongation and orthostatic hypotension.

This review of iloperidone for schizophrenia found it as effective as haloperidol, risperidone, and ziprasidone in reducing symptoms, with similar adverse event and discontinuation rates. Common adverse events are mild (dizziness, hypotension, dry mouth, weight gain). Iloperidone has low propensity for akathisia, extrapyramidal symptoms, prolactin elevation, or metabolic changes. It prevents relapse similarly to haloperidol and allows easy switching from prior antipsychotics. Iloperidone is promising, particularly for patients intolerant to other antipsychotics, though cost-effectiveness comparisons are needed.

Fig. 1 Flowchart of the systematic review process and final included studies. (Tonin FS, et al., 2016)

References

Tonin FS, et al. Iloperidone in the treatment of schizophrenia: an evidence-based review of its place in therapy. Core Evid. 2016;11:49-61.

Does Iloperidone require protection from light during long‑term storage?

Yes, it is photosensitive. Light exposure can cause photodegradation of the oxazolidinone ring. Store in light‑resistant containers, preferably amber glass or original packaging.

What is the recommended storage temperature for Iloperidone?

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

Is Iloperidone hygroscopic, and how is this managed?

It is slightly hygroscopic. Under high humidity (>70% RH), it may absorb moisture and clump. Storage in tightly sealed containers with desiccant is recommended.

How is the impurity iloperidone 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.