iptacopan

Contraindicated in:

Hypersensitivity;
Unresolved serious infection caused by encapsulated bacteria, including Streptococcus pneumoniae, Neisseria meningitidis, or Haemophilus influenzae type B;
Severe renal impairment;
Severe hepatic impairment;
Lactation: Lactation.

Use Cautiously in:

OB: Safety not established in pregnancy;
Pedi: Safety and effectiveness not established in children.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension

Derm: rash, urticaria

EENT: nasopharyngitis

GI: abdominal pain, diarrhea, nausea

Hemat: thrombocytopenia

Metab: hyperlipidemia

MS: arthralgia

Neuro: headache, dizziness

Misc: INFECTION (INCLUDING NEISSERIA MENINGITIDIS, STREPTOCOCCUS PNEUMONIAE, AND HAEMOPHILUS INFLUENZAE TYPE B)Neisseria meningitidis, Streptococcus pneumoniae, and Haemophilus influenzae type B)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP2C8 inhibitors, including gemfibrozil, may ↑ levels and risk of toxicity; concurrent use not recommended.
CYP2C8 inducers, including rifampin, may ↓ levels and effectiveness.

Availability ⬆ ⬇

Capsules: 200 mg

Route/Dosage ⬆ ⬇

PO (Adults ): 200 mg twice daily.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Binds to factor B of the alternative complement pathway and regulates the cleavage of C3, generation of downstream effectors, and amplification of the terminal pathway, which ultimately controls both intravascular and extravascular hemolysis.

Therapeutic effects:

Increase in hemoglobin concentrations and reduction in need for transfusions in PNH.
Reduction in proteinuria in primary immunoglobulin A nephropathy.

Classifications ⬆ ⬇

Therapeutic Classification: none assigned

Pharmacologic Classification: complement.inhibitors

Pharmacokinetics ⬆ ⬇

Absorption: Unknown.

Distribution: Well distributed to tissues.

Protein Binding: 75–93%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP2C8 isoenzyme with some contribution by CYP2D6. Also undergoes glucuronidation via UGT1A1, UGT1A3, and UGT1A8. Primarily excreted in the feces (71.5%; 17% as unchanged drug), with 24.8% being excreted in the urine (18% as unchanged drug).

Half-Life: 25 hr.

Time/Action Profile ⬆ ⬇

(plasma concentrations)

ROUTE	ONSET	PEAK	DURATION
PO	rapid	2 hr	unknown

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication. Advise patient to read Patient Information and REMS educational materials before starting therapy.
Inform patients with PNH of the importance of taking iptacopan as prescribed to ↓ hemolysis risk.
Advise patient to carry Patient Safety Card at all times during and for 2 wk after therapy completion.
Counsel on ↑ risk of meningococcal infection and the need to take vaccines and antibiotics as indicated. Advise patient that vaccination may not prevent serious infection and to notify health care professional at 1st signs of meningococcal infection (fever, rash, stiff neck/back, muscle aches, headache, confusion, photosensitivity, nausea, vomiting) or other infection, including upper respiratory infection.
Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking other medications.
Rep: Advise patient regarding fetal and maternal risks of untreated PNH or immunoglobulin A nephropathy including ↑ mortality in both. Notify health care professional if pregnancy is planned or suspected or if breastfeeding. Advise patient to avoid breastfeeding during therapy and for 5 days after last dose.

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Indications ⬇

Contraind./Precautions ⬆ ⬇