TEVIMBRA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for TEVIMBRA (TEVIMBRA).
Tevimbra (tislelizumab) is a humanized monoclonal antibody that binds to the programmed death-1 (PD-1) receptor and blocks its interaction with ligands PD-L1 and PD-L2, thereby releasing PD-1 pathway-mediated inhibition of the immune response, including the anti-tumor immune response. This restores T cell effector function and enhances immune-mediated killing of tumor cells.
| Metabolism | Tislelizumab is a monoclonal antibody; it is expected to be degraded into small peptides and amino acids via general protein catabolism. No specific metabolic pathways or CYP enzymes are involved. |
| Excretion | Primarily degraded via catabolism; no significant renal or biliary excretion. Elimination via reticuloendothelial system. |
| Half-life | Terminal half-life approximately 21.5 days (range 14–30 days), supporting every-3-week dosing interval. |
| Protein binding | >90% bound, primarily to albumin and to a lesser extent to alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd approximately 5–6 L, indicating limited distribution outside plasma and interstitial space; not extensively distributed into tissues. |
| Bioavailability | Not applicable for IV administration; bioavailability is 100% via IV route. |
| Onset of Action | Following IV infusion, pharmacodynamic effects (T-cell activation) observed within 24–48 hours; clinical response may take weeks to months. |
| Duration of Action | Duration of target engagement persists for several weeks post-dose due to long half-life; clinical effect duration varies with tumor response and immune-related adverse events. |
200 mg intravenously every 3 weeks or 400 mg intravenously every 6 weeks.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment recommended for mild to moderate renal impairment. Insufficient data for severe renal impairment. |
| Liver impairment | No dose adjustment recommended for mild hepatic impairment (Child-Pugh A). Not recommended for moderate or severe hepatic impairment (Child-Pugh B or C). |
| Pediatric use | Safety and efficacy not established in pediatric patients. |
| Geriatric use | No dose adjustment recommended for patients ≥65 years. Monitor for adverse events due to potential age-related comorbidities. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for TEVIMBRA (TEVIMBRA).
| Breastfeeding | It is not known whether tislelizumab is excreted in human milk. However, most monoclonal antibodies are excreted in breast milk in low amounts, especially during the early postpartum period. The M/P ratio is unknown. Given the potential for adverse reactions in the breastfed infant, including immunosuppression, breastfeeding is not recommended during treatment and for at least 5 half-lives (approximately 3 months) after the last dose. |
| Teratogenic Risk | TEVIMBRA (tislelizumab) is an anti-PD-1 monoclonal antibody. Based on its mechanism of action (checkpoint inhibition), there is a potential risk of fetal harm due to increased risk of immune-mediated rejection of the fetus. IgG antibodies cross the placenta; the risk is highest during the second and third trimesters. No adequate human data are available; animal studies have not been conducted. The drug should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Fetal risks include increased rates of abortion, stillbirth, preterm birth, and low birth weight. Immune-related adverse effects in the neonate are possible. |
■ FDA Black Box Warning
None. Tevimbra does not have a black box warning.
| Serious Effects |
["None known"]
| Precautions | ["Immune-mediated adverse reactions: including pneumonitis, colitis, hepatitis, endocrinopathies, nephritis, dermatologic reactions, and myocarditis","Infusion-related reactions","Complications of allogeneic hematopoietic stem cell transplantation (HSCT) after PD-1 blockade","Embryo-fetal toxicity"] |
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| Fetal Monitoring | Monitor maternal thyroid function, hepatic function, and for immune-related adverse events including colitis, hepatitis, pneumonitis, and dermatitis. Fetal monitoring includes ultrasound for growth parameters, amniotic fluid volume, and fetal wellbeing due to risks of intrauterine growth restriction and preterm labor. Consider monitoring for neonatal immune-mediated adverse effects after delivery. |
| Fertility Effects | Based on animal studies for other anti-PD-1 antibodies, tislelizumab may impair fertility in females due to altered immune regulation of reproductive tissues. Amenorrhea or ovarian failure may occur. No specific human data are available for tislelizumab. The effect on male fertility is unknown. Advise patients of potential risks to reproductive capacity. |