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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
Brands: Lucentis


Recombinant humanized immunoglobulin G1 kappa (IgG1 kappa) monoclonal antibody fragment; a vascular endothelial growth factor A (VEGF-A) antagonist.1 3 4 5 6

Uses for Ranibizumab

Neovascular Age-related Macular Degeneration

Treatment of neovascular (wet) age-related macular degeneration.1 4

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Ranibizumab Dosage and Administration


Ophthalmic 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
Ophthalmic Administration

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

Special Populations

Renal and Hepatic Impairment

Dosage adjustment not expected to be necessary.1 (See Hepatic Impairment and also Renal Impairment under Cautions.)

Geriatric Patients

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.)

Traumatic cataract reported rarely.1 4 5

Increased IOP

Increased IOP observed within 60 minutes of intravitreal injection.1 4 6 Monitor IOP and perfusion of optic nerve head and manage appropriately.1 4

Thromboembolic Events

Arterial thromboembolic events reported.1 5 Potential risk of arterial thromboembolic events following intravitreal injection of VEGF antagonists.1


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

General Precautions


Development of low-titer antibodies reported.1 Clinical relevance unclear, but iritis or vitritis noted in some patients with the highest levels of immunoreactivity.1

Specific Populations


Category C.1


Not known whether ranibizumab is distributed into milk.1 Caution if used in nursing women.1

Pediatric Use

Safety and efficacy not established.1

Adult Use

Safety and efficacy not established in adults <50 years of age.4

Geriatric Use

No substantial differences in efficacy or systemic exposure (after correcting for Clcr) relative to younger adults.1

Hepatic Impairment

Pharmacokinetics not studied; dosage adjustment not expected to be necessary.1

Renal Impairment

Pharmacokinetics not studied; however, limited data indicate clearance not substantially affected by renal impairment.1 Dosage adjustment not expected to be necessary.1

Common Adverse Effects

Conjunctival hemorrhage,1 4 eye pain,1 4 vitreous floaters,1 4 increased IOP,1 4 intraocular inflammation.1 4

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

Ranibizumab Pharmacokinetics



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





2–8°C.1 Do not freeze; protect from light.1 Store in original carton until use.1


  • Binds to active forms of human VEGF-A, including cleaved form (VEGF110), and inhibits their biologic activity.1 3 4

  • 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

  • Risk of developing endophthalmitis.1 Importance of informing ophthalmologist immediately if change in vision occurs or if treated eye becomes red, sensitive to light, or painful.1

  • 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.

Ranibizumab (Recombinant)


Dosage Forms


Brand Names



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)


AHFS DI Essentials. © Copyright, 2004-2015, 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]