Immune thrombocytopenia (ITP)

Active Ingredient: Rilzabrutinib

Indication for Rilzabrutinib

Population group: only adults (18 years old or older)
Therapeutic intent: Curative procedure

Rilzabrutinib is indicated for the treatment of immune thrombocytopenia (ITP) in adult patients who are refractory to other treatments.

For this indication, competent medicine agencies globally authorize below treatments:

400 mg twice daily

For:

Dosage regimens

Oral, 400 milligrams rilzabrutinib, 2 times daily.

Detailed description

The recommended dose of rilzabrutinib is 400 mg twice daily.

Use with CYP3A inhibitors or inducers and gastric acid reducing agents

Recommended use with cytochrome P450 enzyme 3A (CYP3A) inhibitors or inducers and gastric acid reducing agents are provided in the following table.

Use with CYP3A inhibitors or inducers and gastric acid reducing agents:

 Co-administered medicinal productRecommended use
CYP3A inhibitorsStrong and moderate CYP3A inhibitorAvoid co-administration of
rilzabrutinib with moderate or
strong CYP3A inhibitors. If
these inhibitors will be used
short-term (such as anti-
infectives for up to seven
days), interrupt rilzabrutinib.
Avoid co-administration of
grapefruit, starfruit and
products containing these
fruits, and Seville oranges with
rilzabrutinib, as these are
moderate or strong inhibitors of
CYP3A.
Weak CYP3A inhibitorNo dose adjustment.
CYP3A inducersStrong and moderate CYP3A inducersAvoid co-administration of
rilzabrutinib with moderate or
strong CYP3A inducers.
Weak CYP3A inducerNo dose adjustment.
Gastric acid
reducing agents
Proton pump inhibitors (PPIs)Avoid co-administration of
rilzabrutinib with PPIs.
H2-receptor antagonists or antacidIf treatment with a gastric acid
reducing agent is required,
consider using a H2-receptor
antagonist (H2RA) or antacid.
Take rilzabrutinib at least
2 hours before taking the
H2RA or antacid.

Missed dose

If a dose of rilzabrutinib is missed, patients should take the missed dose as soon as possible on the same day with a return to the regular schedule the following day. The missed dose and the next regular scheduled dose must be taken more than 2 hours apart. Extra doses should not be taken to make up for the missed dose.

Discontinuation

Treatment with rilzabrutinib should be discontinued after 12 weeks of rilzabrutinib therapy if the platelet count does not increase to a level sufficient to avoid clinically important bleeding.

Dosage considerations

The tablets can be taken at approximately the same time each day with or without food. In patients who experience gastrointestinal symptoms, taking rilzabrutinib with food may improve tolerability.

Active ingredient

Rilzabrutinib

Rilzabrutinib is a selective, covalent, reversible inhibitor of Bruton's tyrosine kinase (BTK), with a tailored residence time at BTK to reduce off-target effects. In immune thrombocytopenia (ITP), rilzabrutinib mediates its therapeutic effect through multi-immune modulation by inhibiting B cell activation, interruption of FcγR mediated phagocytosis, and potentially amelioration of chronic inflammation associated with ITP.

Read more about Rilzabrutinib

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