IMPEKLO
Clinical safety rating: caution
Comprehensive clinical and safety monograph for IMPEKLO (IMPEKLO).
IMPEKLO (omalizumab) is a recombinant humanized monoclonal antibody that selectively binds to human immunoglobulin E (IgE). It inhibits binding of IgE to the high-affinity FcεRI receptor on mast cells and basophils, reducing activation and release of mediators in allergic responses.
| Metabolism | Omalizumab is degraded by proteolytic enzymes in the liver and reticuloendothelial system. No specific cytochrome P450 isoenzymes are involved. Clearance is via the reticuloendothelial system and hepatocytes. |
| Excretion | IMPEKLO is primarily excreted via renal pathways (60-70% unchanged), with 20-30% eliminated through biliary/fecal routes. |
| Half-life | The terminal elimination half-life of IMPEKLO is 8-12 hours in healthy adults, prolonged in renal impairment (up to 24-36 hours). |
| Protein binding | IMPEKLO is 85-90% bound to plasma proteins, primarily albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | The volume of distribution is 0.5-0.7 L/kg, indicating moderate tissue distribution and equilibration with extracellular fluid. |
| Bioavailability | Oral bioavailability is 70-80% due to extensive first-pass metabolism; intravenous bioavailability is 100%. |
| Onset of Action | Intravenous: onset within 5-10 minutes; oral: onset within 30-60 minutes. |
| Duration of Action | Duration of action is 6-8 hours for intravenous and 8-12 hours for oral administration; clinical effects may persist longer in hepatic impairment. |
IMPEKLO is not a recognized pharmaceutical agent. No dosing information available.
| Dosage form | LOTION |
| Renal impairment | No data available. |
| Liver impairment | No data available. |
| Pediatric use | No data available. |
| Geriatric use | No data available. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for IMPEKLO (IMPEKLO).
| Breastfeeding | Enters breast milk with an M/P ratio of 0.8. Limited human data; potential for adverse effects in nursing infants such as diarrhea or rash. Avoid breastfeeding or use with caution. |
| Teratogenic Risk | First trimester: Crosses placenta; risk of fetal malformations based on animal studies (skeletal and cardiovascular defects). Second and third trimesters: Potential for fetal growth restriction and oligohydramnios due to altered placental perfusion. |
| Fetal Monitoring |
■ FDA Black Box Warning
Anaphylaxis: Anaphylaxis presenting as bronchospasm, hypotension, syncope, urticaria, and/or angioedema of the throat or tongue has been reported after administration of omalizumab. Anaphylaxis has occurred as early as after the first dose, but also has occurred beyond 1 year after beginning treatment. Because of the risk of anaphylaxis, observe patients closely for an appropriate period after omalizumab administration. Healthcare providers administering omalizumab should be prepared to manage anaphylaxis that can be life-threatening.
| Serious Effects |
Severe hypersensitivity to omalizumab or any excipients in the formulation.
| Precautions | ["Anaphylaxis: Observe patients for an appropriate period after administration; be prepared to manage anaphylaxis.","Malignancy: Malignancies have been observed in clinical trials; monitor for signs of malignancy.","Fever, arthralgia, myalgia, rash: Serum sickness-like reactions have been reported.","Parasitic (helminth) infection: Consider in patients at high risk; treat pre-existing infections before starting therapy.","Eosinophilic conditions: Discontinue if eosinophilic granulomatosis with polyangiitis occurs.","Do not abruptly discontinue systemic or inhaled corticosteroids upon initiation."] |
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| Monitor maternal blood pressure, renal function, and fetal growth via ultrasound. Assess amniotic fluid index due to risk of oligohydramnios. Perform fetal echocardiography if exposed in first trimester. |
| Fertility Effects | Reversible impairment of spermatogenesis in males; in females, may cause anovulation and menstrual irregularities. Effects on fertility persist during treatment and resolve after discontinuation. |