ENTYVIO
Clinical safety rating
cautionComprehensive clinical and safety monograph for ENTYVIO (ENTYVIO).
Comprehensive clinical and safety monograph for ENTYVIO (ENTYVIO).
Adult patients with moderately to severely active ulcerative colitis (UC) for inducing and maintaining clinical response and remission, and achieving mucosal healingAdult patients with moderately to severely active Crohn's disease (CD) for inducing and maintaining clinical response and remission, and achieving mucosal healingOff-label: Treatment of chronic pouchitis, graft-versus-host disease (GVHD) involving the gastrointestinal tract
Vedolizumab is a humanized monoclonal antibody that binds to the α4β7 integrin, blocking its interaction with mucosal addressin cell adhesion molecule-1 (MAdCAM-1). This inhibits the migration of memory T-lymphocytes into the gastrointestinal tract, reducing inflammation.
| Metabolism | Vedolizumab is a monoclonal antibody degraded into small peptides and amino acids via general protein catabolism. It is not metabolized by cytochrome P450 enzymes. |
| Excretion | Primarily eliminated via hepatic catabolism into small peptides and amino acids; <0.15% of dose excreted unchanged in urine; no significant biliary/fecal excretion of intact drug. |
| Half-life | Terminal half-life approximately 25 days (range 18–31 days) in patients with ulcerative colitis, supporting every-8-week maintenance dosing. |
| Protein binding | Approximately 95% bound to serum proteins, primarily albumin. |
| Volume of Distribution | Central volume ~2.5 L; total volume of distribution ~5.0 L (approx. 0.07 L/kg for a 70 kg patient), indicating predominant distribution in the vascular space. |
| Bioavailability | IV only (100% bioavailability); no data for oral or other routes as it is not administered via those routes. |
| Onset of Action | IV: Clinical response may be observed within 2–6 weeks after initiation of therapy; maximal effect by 6–10 weeks. |
| Duration of Action | Duration of therapeutic effect persists for approximately 8 weeks after IV infusion, aligning with recommended dosing interval; notable interindividual variability. |
| Molecular Weight | 146833 |
300 mg intravenous infusion over 30 minutes at weeks 0, 2, and 6, then every 8 weeks thereafter.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for renal impairment. |
| Liver impairment | No dose adjustment required for hepatic impairment. |
| Pediatric use | Not approved for pediatric use; safety and efficacy not established. |
| Geriatric use | No specific dose adjustment; use with caution due to limited data in elderly. |
| 1st trimester | Limited data; human IgG crosses placenta; potential risk unknown. Use only if clearly needed. |
| 2nd trimester | Human IgG crosses placenta; fetal exposure increases after 13 weeks. Consider maternal benefit vs fetal risk. |
| 3rd trimester | Human IgG crosses placenta readily; may affect infant immune response. Avoid near term unless essential. |
Clinical note
Comprehensive clinical and safety monograph for ENTYVIO (ENTYVIO).
| Placental transfer | Human IgG monoclonal antibody; crosses placenta via FcRn-mediated transport, especially in second and third trimesters. Fetal concentrations may exceed maternal levels. |
| Breastfeeding | Vedolizumab is excreted in human milk at low levels; consider the developmental and health benefits of breastfeeding along with the mother's clinical need for the drug and any potential adverse effects on the breastfed child from the drug or the underlying maternal condition. |
| Lactation Rating | L3 |
| Teratogenic Risk | Entyvio (vedolizumab) is an IgG1 monoclonal antibody. IgG crosses the placenta in an increasing fashion during the second and third trimesters. Available data from a small number of pregnancies in women with inflammatory bowel disease (IBD) are insufficient to inform a drug-associated risk for major birth defects or miscarriage. In animal reproductive studies, no adverse developmental effects were observed in offspring of pregnant cynomolgus monkeys administered intravenous vedolizumab during organogenesis at doses up to 100 mg/kg (approximately 20 times the recommended human dose). However, because of the potential for IgG transport, vedolizumab may be transmitted from the mother to the developing fetus, particularly in the third trimester. Therefore, the risk to the fetus cannot be excluded. |
| Fetal Monitoring | Monitor for infections in both mother and infant, as vedolizumab may increase the risk of infections. For infants exposed in utero, particularly in the third trimester, monitor for signs of infections, especially opportunistic infections. No specific routine fetal monitoring is required, but standard prenatal care should be maintained. Consider checking vedolizumab serum levels in the infant if clinically indicated, as vedolizumab may persist in the infant's circulation for several months after birth. |
| Fertility Effects | No human data are available on the effect of vedolizumab on fertility. In animal studies, no adverse effects on male or female fertility were observed in mice treated with an analogous anti-human α4β7 integrin antibody at doses up to 100 mg/kg. |
■ FDA Black Box Warning
Progressive multifocal leukoencephalopathy (PML) has been reported with vedolizumab. PML is an opportunistic viral infection of the brain caused by the JC virus that typically leads to severe disability or death. Monitor patients for any new or worsening neurological signs or symptoms.
| Serious Effects |
Hypersensitivity to vedolizumab or any excipientsActive severe infections (e.g., tuberculosis, sepsis, opportunistic infections)
| Precautions | Increased risk of infections, including serious infections such as tuberculosis, sepsis, and opportunistic infections, Progressive multifocal leukoencephalopathy (PML) risk, Hypersensitivity reactions including anaphylaxis and infusion-related reactions, Hepatic injury: Elevated liver enzymes and bilirubin have been reported, Interference with laboratory tests: Vedolizumab may falsely elevate total protein and albumin levels by binding to reagents in certain assays |
| Food/Dietary | No known food interactions. No dietary restrictions required. |
| Clinical Pearls | ENTYVIO (vedolizumab) is a gut-selective integrin antagonist; do not co-administer with natalizumab or TNF-alpha inhibitors due to increased infection risk. Live vaccines should be given at least 30 days prior to initiation. Infusion-related reactions are uncommon but monitor during infusion. No significant drug interactions with CYP450 substrates. |
| Patient Advice | Inform your doctor if you have a history of infections, TB, or recent live vaccines. · Report any signs of infusion reaction (hives, itching, difficulty breathing, dizziness) during or after infusion. · Avoid live vaccines during treatment and for at least 30 days after last dose. · ENTYVIO may increase risk of serious infections; contact doctor if you develop fever, cough, or other infection symptoms. · Take all doses as scheduled; do not skip infusions even if you feel well. |
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