Overview
11 DESCRIPTION Zilucoplan, a complement inhibitor, is a 15 amino-acid, synthetic macrocyclic peptide. The molecular formula of zilucoplan is C 172 H 278 N 24 O 55 in free acid form and its molecular weight is 3562.23 Daltons (free acid form). The chemical name for zilucoplan sodium is: acetyl‐[L-lysyl 1 -L-valyl 2 -L-glutamyl 3 -L-arginyl 4 -L phenylalanyl 5 -L aspartyl 6 ]- N -methyl L-aspartyl...
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Zilucoplan binds to the complement protein C5 and inhibits its cleavage to C5a and C5b, preventing the generation of the terminal complement complex, C5b-9. The precise mechanism by which zilucoplan exerts its therapeutic effect in generalized myasthenia gravis is unknown but is presumed to involve reduction of C5b-9 deposition at the neuromuscular junction. 12.2 Pharmacodynamics In a placebo-controlled Phase 2 study, patients received zilucoplan 0.3 mg/kg or 0.1 mg/kg for 12 weeks. There was a dose dependent inhibition of complement. Complement inhibition as represented by inhibition of sheep red blood cell (sRBC) lysis was 89.1% within 3 hours after the first administration and 94.
Indications
- 1 INDICATIONS AND USAGE ZILBRYSQ is indicated for the treatment of generalized myasthenia gravis (gMG) in adult patients who are anti-acetylcholine receptor (AChR) antibody positive. ZILBRYSQ is a complement inhibitor indicated for the treatment of generalized myasthenia gravis (gMG) in adult patients who are anti-acetylcholine receptor (AChR) antibody positive. ( 1 )
Common Doses
- 16.6 mg
- 23 mg
- 32.4 mg
Dosage
2 DOSAGE AND ADMINISTRATION Obtain baseline amylase and lipase. ( 2.2 ) For subcutaneous injection only. ( 2.3 ) Recommended dosage ( 2.3 ): Body Weight Once Daily Dosage Plunger Rod Color of Prefilled Syringe Less than 56 kg 16.6 mg RUBINE RED 56 kg to less than 77 kg 23 mg ORANGE 77 kg and above 32.4 mg DARK BLUE See Full Prescribing Information for instructions on dosage, preparation, and administration. ( 2.4 , 2.5 ) 2.
Black Box Warning
WARNING: SERIOUS MENINGOCOCCAL INFECTIONS ZILBRYSQ, a complement inhibitor, increases the risk of serious infections caused by Neisseria meningitidis [see Warnings and Precautions (5.1) ] . Life-threatening and fatal meningococcal infections have occurred in patients treated with complement inhibitors. These infections may become rapidly life-threatening or fatal if not recognized and treated early. Complete or update vaccination for meningococcal bacteria (for serogroups A, C, W, Y, and B) at least 2 weeks prior to the first dose of ZILBRYSQ, unless the risks of delaying therapy outweigh the...
Contraindications
- 4 CONTRAINDICATIONS ZILBRYSQ is contraindicated for initiation in patients with unresolved serious Neisseria meningitidis infection [see Warnings and Precautions (5.1) ] . ZILBRYSQ is contraindicated for initiation in patients with unresolved serious Neisseria meningitidis infection. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following clinically significant adverse reactions are discussed in greater detail in other sections of the labeling: Serious Meningococcal Infections [see Warnings and Precautions (5.1) ] Other Infections [see Warnings and Precautions (5.3) ] Pancreatitis and Other Pancreatic Conditions [see Warnings and Precautions (5.4) ] The most common adverse reactions (≥10%) in patients with gMG were injection site reactions, upper respiratory tract infection, and diarrhea. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact UCB, Inc.
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.