Class: EENT Drugs, Miscellaneous
VA Class: OP900
Chemical Name: Disulfide with human-mouse monoclonal rhuFAB V2 light chain anti-(human vascular endothelial growth factor) Fab fragment (human-mouse monoclonal rhuFAB V2 γ1-chain) immunoglobulin G1
Molecular Formula: C2158H3282N562O681 S12
CAS Number: 347396-82-1
Uses for Ranibizumab
Neovascular Age-related Macular Degeneration
Ranibizumab Dosage and Administration
Administer by intravitreal injection only into the affected eye(s).1
Prior to intravitreal administration, withdraw entire contents (0.2 mL) of ranibizumab injection through a sterile 5-micron, 19-gauge filter needle (provided by manufacturer) into a 1-mL tuberculin syringe using aseptic technique.1 4 Next, replace filter needle with a sterile 30-gauge, ½-inch needle (provided by manufacturer) for intravitreal injection.1 To obtain appropriate dose (0.5 mg), expel contents in tuberculin syringe until plunger tip is aligned with the line that marks 0.05 mL on the syringe.1
Inject under controlled aseptic conditions (including use of sterile gloves, sterile drape, a sterile eyelid speculum [or equivalent]) following adequate anesthesia and administration of a broad-spectrum anti-infective agent.1
Monitor patients for elevation of IOP and for development of endophthalmitis following intravitreal injection.1 Monitoring for increased IOP may include evaluation of optic nerve head perfusion immediately after injection, tonometry within 30 minutes following injection, and biomicroscopy between 2–7 days following injection.1
Each vial should be used only for treatment of a single eye.1 If contralateral eye requires treatment, use a new vial; change sterile field, syringe, gloves, drape, eyelid speculum, and filter and injection needles before administering to the other eye.1
Neovascular Age-related Macular Degeneration
Intravitreal injection: 0.5 mg (0.05 mL) into the affected eye(s) once every month (approximately 28 days).1
After first 4 injections, may reduce dosage to one injection every 3 months if monthly injections are not feasible; however, because this reduced dosage is less effective in maintaining visual acuity, evaluate patients regularly.1
Safety and efficacy beyond 2 years of therapy not established.1
Renal and Hepatic Impairment
Dosage adjustment not expected to be necessary.1 (See Hepatic Impairment and also Renal Impairment under Cautions.)
No dosage adjustment required.1
Cautions for Ranibizumab
Ocular or periocular infections.1
Known hypersensitivity (e.g., severe intraocular inflammation) to ranibizumab or any ingredient in the formulation.1
Endophthalmitis and Other Serious Ocular Effects
Intravitreal injections, including those with ranibizumab, associated with endophthalmitis and retinal detachments.1 4 5 6 Always use proper aseptic injection technique.1 4 (See Ophthalmic Administration under Dosage and Administration.) Monitor patients closely for signs of endophthalmitis (e.g., redness, sensitivity to light, pain, changes in vision) during the week following injection to permit early treatment.1 4 (See Advice to Patients.)
According to interim safety analysis of an ongoing study (SAILOR study), incidence of stroke appeared to be higher with 0.5-mg dose than with 0.3-mg dose.7 8 Patients with prior history of stroke appeared to be at increased risk for a subsequent stroke.7
Safety and efficacy not established.1
Safety and efficacy not established in adults <50 years of age.4
No substantial differences in efficacy or systemic exposure (after correcting for Clcr) relative to younger adults.1
Pharmacokinetics not studied; dosage adjustment not expected to be necessary.1
Common Adverse Effects
Interactions for Ranibizumab
No formal drug interaction studies to date.1
Photodynamic Therapy with Verteporfin
Serious intraocular inflammation reported; most cases occurred when ranibizumab was administered approximately 7 days after verteporfin photodynamic therapy.1
Following monthly intravitreal injection, peak serum concentrations attained were substantially below that necessary to inhibit the biologic activity of VEGF-A by 50%.1 Serum concentrations predicted to be approximately 90,000 times lower than vitreal concentrations.1
Peak serum concentrations predicted to be reached approximately 1 day after monthly intravitreal administration of 0.5 mg per eye.1
Estimated average vitreous half-life: Approximately 9 days.1
VEGF-A induces neovascularization (angiogenesis) and increases vascular permeability, which appears to play a role in the pathogenesis and progression of neovascular (wet) age-related macular degeneration,1 3 4 a leading cause of blindness in adults >60 years of age in developed countries.2 3 4
Binding to VEGF-A prevents VEGF-A from binding to VEGF receptors (i.e., VEGFR-1, VEGFR-2) on the surface of endothelial cells, reducing endothelial cell proliferation, angiogenesis, and vascular permeability.1 4
Shown to reduce foveal retinal thickening and vascular permeability associated with age-related macular degeneration; however, foveal retinal thickness data did not provide information useful in influencing treatment decisions, and the area of vascular permeability was not correlated with visual acuity.1
Advice to Patients
Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed.1
Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses (e.g., ocular or periocular infections).1
Importance of informing patients of other important precautionary information. (See Cautions.)
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Injection, for intravitreal use only
10 mg/mL (0.5 mg/0.05 mL)
Lucentis (preservative-free; available as single-dose vial with filter and injection needles)
This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.
The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.
AHFS Drug Information. © Copyright, 1959-2013, Selected Revisions April 1, 2010. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
1. Genentech, Inc. Lucentis (ranibizumab) injection prescribing information. South San Francisco, CA; 2008 Apr.
2. World Health Organization. Magnitude and causes of visual impairment. Fact Sheet No. 282; 2004 Nov. From WHO website (). Accessed 2006 Sep 13.
3. Rosenfeld PJ, Rich RM, and Lalwani GA. Ranibizumab: Phase III clinical trial results. Ophthalmol Clin N Am. 2006; 19:361-72.
4. Genentech, Inc, South San Francisco, CA: Personal communication.
5. Brown DM, Kaiser PK, Michels M et al for the ANCHOR Study Group. Ranibizumab versus verteporfin for neovascular age-related macular degeneration. N Engl J Med. 2006; 355:1432-44. [PubMed 17021319]
6. Rosenfeld PJ, Brown DM, Heier JS et al for the MARINA Study Group. Ranibizumab for neovascular age-related macular degeneration. N Engl J Med. 2006; 355:1419-31. [PubMed 17021318]
7. Barron H. Dear healthcare provider letter: important safety information about Lucentis. South San Francisco, CA: Genentech, Inc.; 2007 Jan 24.
8. Food and Drug Administration. Lucentis (ranibizumab injection) [February 1, 2007]. Medwatch alert. Rockville, MD; February 2007. From FDA website (). (Accessed 2009 Oct 12.)
9. Brown DM, Michels M, Kaiser PK et al. Ranibizumab versus verteporfin photodynamic therapy for neovascular age-related macular degeneration: Two-year results of the ANCHOR study. Ophthalmology. 2009; 116:57-65. [PubMed 19118696]