AVASTIN
Clinical safety rating: caution
Comprehensive clinical and safety monograph for AVASTIN (AVASTIN).
Bevacizumab is a recombinant humanized monoclonal antibody that binds to vascular endothelial growth factor (VEGF) and inhibits its interaction with VEGF receptors (VEGFR-1 and VEGFR-2) on the surface of endothelial cells, thereby inhibiting angiogenesis and tumor growth.
| Metabolism | Bevacizumab is primarily metabolized via proteolytic degradation into small peptides and amino acids. No specific metabolic enzymes are involved; it is not metabolized by cytochrome P450 enzymes. |
| Excretion | Primarily via reticuloendothelial system and proteolytic catabolism; negligible renal excretion (<1% unchanged in urine) |
| Half-life | Terminal half-life approximately 20 days (range 11–50 days) in patients; supports dosing every 2–3 weeks |
| Protein binding | Bound primarily to albumin and other plasma proteins; approximately 95–100% bound (saturable binding to FcRn may occur) |
| Volume of Distribution | Vd approximately 2.9–3.7 L (not weight-normalized; small Vd consistent with large monoclonal antibody confined mainly to plasma and interstitial space) |
| Bioavailability | Only available as intravenous infusion; bioavailability 100% by IV route; not administered subcutaneously or orally (no bioavailability data for other routes) |
| Onset of Action | Intravenous: Onset within 2–3 weeks (based on tumor response and vascular normalization) |
| Duration of Action | Sustained VEGF suppression for at least 4 weeks after single dose; clinical effect duration correlates with half-life and dosing interval |
| Action Class | Vascular endothelial growth factor (VEGF) inhibitor |
| Brand Substitutes | Bevnexxa 100mg Injection, Advamab 100mg Injection, Krabeva 100mg Injection, Bevacirel 100mg Injection, Bevarest 100mg Injection, Abevmy 400mg Injection, Krabeva 400mg Injection, Avangio Injection, Vegfxta 400mg Injection, Advamab 400 Injection |
5 mg/kg intravenously every 2 weeks or 7.5 mg/kg intravenously every 3 weeks for metastatic colorectal cancer; 10 mg/kg intravenously every 2 weeks for non-small cell lung cancer; 15 mg/kg intravenously every 3 weeks for glioblastoma; 15 mg/kg intravenously every 3 weeks for metastatic renal cell carcinoma (in combination with interferon alfa).
| Dosage form | VIAL |
| Renal impairment | No dose adjustment is recommended for patients with renal impairment; however, be cautious in severe renal impairment (GFR <30 mL/min) due to limited data. |
| Liver impairment | No specific dose adjustment guidelines exist for hepatic impairment based on Child-Pugh score; use with caution in severe hepatic impairment. |
| Pediatric use | Safety and efficacy in pediatric patients have not been established; no standard dosing guidelines available. |
| Geriatric use | No specific dose adjustment is required for elderly patients; however, monitor for increased incidence of arterial thromboembolic events, hypertension, and proteinuria as seen in clinical trials. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for AVASTIN (AVASTIN).
| Breastfeeding | No data on excretion in human milk. M/P ratio unknown. Due to potential for adverse effects in nursing infants, breastfeeding is not recommended during therapy and for at least 6 months after last dose. |
| Teratogenic Risk | Pregnancy Category C. First trimester: Risk of fetal malformations based on animal studies; no adequate human studies. Second and third trimesters: Oligohydramnios, fetal renal impairment, and spontaneous abortion reported. Avoid use unless potential benefit justifies risk. |
| Fetal Monitoring |
■ FDA Black Box Warning
WARNING: GASTROINTESTINAL PERFORATIONS, SURGERY AND WOUND HEALING COMPLICATIONS, and HEMORRHAGE. Gastrointestinal perforations occur in up to 2.4% of patients. Discontinue for perforations, tracheoesophageal fistula, or wound dehiscence. Severe or fatal hemorrhage, including hemoptysis and gastrointestinal bleeding, has occurred; monitor for bleeding.
| Serious Effects |
["Known hypersensitivity to bevacizumab or any components of the formulation","Recent hemoptysis (≥2.5 mL of red blood) within 21 days prior to treatment","Untreated central nervous system metastases (due to risk of bleeding; treat prior to bevacizumab)"]
| Precautions | ["Gastrointestinal perforations and fistulae (including tracheoesophageal)","Surgery and wound healing complications: do not administer within 28 days of major surgery or until wound is fully healed","Hemorrhage: severe or fatal pulmonary hemorrhage (particularly in squamous NSCLC), gastrointestinal bleeding, and cerebral hemorrhage","Non-gastrointestinal fistula formation (including bronchopleural, biliary, and vaginal)","Arterial thromboembolic events (e.g., stroke, myocardial infarction): risk increased in patients ≥65 years of age","Hypertension: monitor blood pressure; may require antihypertensive therapy","Reversible posterior leukoencephalopathy syndrome (RPLS)","Proteinuria: monitor urine protein; discontinue if nephrotic syndrome develops","Ovarian failure: may impair fertility in women","Congestive heart failure: increased incidence in patients receiving anthracyclines or with prior chest radiation"] |
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| Monitor blood pressure, urine protein, signs of preeclampsia. Perform serial fetal ultrasounds for oligohydramnios. Assess renal function and fluid status. Monitor for hemorrhage in mother and fetus. |
| Fertility Effects | Animal studies show impaired fertility: reduced ovulation, corpus luteum formation, and implantation. Human data limited; may impair female fertility reversibly. Effects on male fertility unknown. |
| Food/Dietary | No specific food interactions known. No restrictions beyond general dietary advice for cancer patients. |
| Clinical Pearls | Monitor blood pressure closely; hypertension is common. Hold therapy 28 days before elective surgery due to impaired wound healing. Use with caution in patients with cardiovascular disease or history of arterial thromboembolism. Proteinuria monitoring required; urine dipstick at baseline and regularly. Avoid in patients with recent hemoptysis or untreated CNS metastases. |
| Patient Advice | Report any signs of bleeding, such as unusual bruising, nosebleeds, or blood in urine/stool. · Inform your doctor immediately if you experience severe headache, vision changes, confusion, or seizures (signs of PRES). · Avoid surgery or dental procedures without notifying your oncologist; therapy may need to be paused. · Females of childbearing age must use effective contraception during and for 6 months after treatment. · Do not drive if you experience vision problems or dizziness from therapy. |