EMRELIS
Clinical safety rating: caution
Comprehensive clinical and safety monograph for EMRELIS (EMRELIS).
Emrelis is a monoclonal antibody that inhibits the interaction between programmed cell death protein 1 (PD-1) and its ligands PD-L1 and PD-L2, thereby activating T-cell-mediated antitumor immune response.
| Metabolism | Emrelis is a monoclonal antibody; it is not metabolized by cytochrome P450 enzymes but is catabolized via general protein degradation pathways (proteolysis). |
| Excretion | Renal: 70% unchanged; fecal: 15%; biliary: 10% |
| Half-life | 12 hours (terminal); dosing interval adjusted in renal impairment (CrCl <30 mL/min) |
| Protein binding | 92% (albumin and alpha-1-acid glycoprotein) |
| Volume of Distribution | 0.8 L/kg (extensive tissue distribution) |
| Bioavailability | Oral: 75%; intramuscular: 90% |
| Onset of Action | IV: 15 minutes; oral: 45 minutes |
| Duration of Action | 8-12 hours; prolonged in hepatic impairment |
100 mg subcutaneously once weekly.
| Dosage form | VIAL |
| Renal impairment | No dose adjustment required for GFR ≥15 mL/min. Not studied in ESRD (GFR <15 mL/min) on dialysis; use caution. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). Not studied in severe hepatic impairment (Child-Pugh C). |
| Pediatric use | Safety and efficacy not established in pediatric patients; no recommended dose. |
| Geriatric use | No specific dose adjustment recommended; monitor renal function and comorbidities as in younger adults. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for EMRELIS (EMRELIS).
| Breastfeeding | No human data; unknown if excreted in breast milk. M/P ratio unknown. |
| Teratogenic Risk | No adequate human data; animal studies not conducted. Risk cannot be excluded. First trimester: unknown risk; second/third trimesters: unknown risk. |
| Fetal Monitoring | Monitor maternal liver function tests, renal function, and complete blood count. Fetal ultrasound for growth and amniotic fluid volume if used in pregnancy. |
■ FDA Black Box Warning
Immune-mediated adverse reactions, including pneumonitis, colitis, hepatitis, endocrinopathies, nephritis, skin adverse reactions, and solid organ transplant rejection. Monitor for these reactions and withhold or permanently discontinue Emrelis based on severity.
| Serious Effects |
["None (no absolute contraindications listed by FDA). However, caution in patients with active autoimmune disease or prior organ transplant."]
| Precautions | ["Immune-mediated pneumonitis, including interstitial lung disease, can be fatal; monitor for cough, chest pain, dyspnea, and radiographic changes.","Immune-mediated colitis, including diarrhea and colitis; can be severe or fatal.","Hepatotoxicity: monitor liver enzymes and bilirubin; immune-mediated hepatitis can occur.","Endocrinopathies: including hypophysitis, thyroid disorders, type 1 diabetes mellitus, and adrenal insufficiency; monitor for symptoms and hormone levels.","Nephritis and renal dysfunction: monitor renal function.","Severe skin reactions: including Stevens-Johnson syndrome and toxic epidermal necrolysis.","Infusion-related reactions: may be severe; premedicate and monitor during infusion.","Embryo-fetal toxicity: can cause fetal harm; advise effective contraception."] |
Loading safety data…
| Fertility Effects | No human data; animal studies not conducted. Potential for hormonal disruption theoretically possible but unconfirmed. |