Reslizumab

Reslizumab is an anti-IL-5 (interleukin-5) belonging to Anti-asthmatic agents

Reslizumab is used in the treatment of Asthma.

Reslizumab is administered intravenously (IV), so it is immediately and completely absorbed into the bloodstream. Reslizumab has a large volume of distribution, indicating that it distributes throughout the body's extracellular fluid. The mean steady-state volume of distribution is approximately 7.5 L.Reslizumab is not metabolized by the liver.Reslizumab is eliminated via proteolytic degradation, mainly in the liver and other tissues. The mean terminal elimination half-life of reslizumab is approximately 24-26 days.

The onset of action of Reslizumab was Within 15-60 minutes.

The Duration of time for Reslizumab was within 2hours.

The Tmax of Reslizumab is approximately 1 to 2 hours after the start of the infusion.

The Cmax of reslizumab, when administered intravenously at a dose of 3 mg/kg, is approximately 50 to 70 micrograms per milliliter (μg/mL).

Reslizumab shows common side effects like Injection site reactions, such as pain, redness, or swelling Headache Fatigue Muscle pain Dizziness

Reslizumab is available in the form of IV Solution.

Reslizumab is available in India, Germany, Canada, Italy, USA

Reslizumab is available in the form of IV Solution.

Reslizumab is used in the treatment of Asthma.

Reslizumab is an interleukin-5 antagonist (IgG4 kappa). IL-5 is the major cytokine responsible for the growth and differentiation, recruitment, activation, and survival of eosinophils (a cell type associated with inflammation and an important component in the pathogenesis of asthma).

Reslizumab is approved for for following clinical indications:-

Asthma, severe eosinophilic: Add-on maintenance treatment of severe asthma in adults with an eosinophilic phenotype.

• Asthma, severe eosinophilic: May consider as add-on therapy in patients with severe eosinophilic asthma inadequately controlled on standard therapies (eg, an inhaled glucocorticoid with a long-acting beta agonist) (Ref). May consider use in patients with peripheral blood eosinophils ≥150 cells/mcL; however, some experts reserve use for patients with peripheral blood eosinophils ≥400 cells/mcL. The eosinophil threshold required for patients on systemic glucocorticoids is less clear.

Reslizumab is available in various strengths as10 ml.

Reslizumab is available in the form of IV Solution.

Hypersensitivity to reslizumab or any component of the formulation.

Concerns related to adverse effects:

• Anaphylaxis:

Anaphylaxis was reported in 0.3% of asthma patients in placebo-controlled studies; these events were observed during or within 20 minutes after completion of infusion, and may occur as early as the second dose. Observe patients for an appropriate period of time after administration. Manifestations included dyspnea, decreased oxygen saturation, wheezing, vomiting, skin and mucosal involvement, including urticaria. If severe systemic reactions, including anaphylaxis occur, discontinue administration immediately and provide appropriate medical treatment.

• Malignancies:

Malignancies were observed during clinical trials with the majority being diagnosed within less than 6 months of drug exposure; neoplasms observed were diverse with no predominant histologic type.

Common Adverse effects:

Injection site reactions, such as pain, redness, or swelling Headache Fatigue Muscle pain Dizziness Itching Upper respiratory tract infections, such as the common cold Nasal congestion Nausea Diarrhea

Less Common Adverse effects:

Allergic reactions, which may include hives, swelling of the face, lips, tongue, or throat, or difficulty breathing Increased risk of infection, including viral or bacterial infections Injection site reactions, such as bruising, bleeding, or infection Low blood cell counts, which may increase your risk of bleeding or infection Hypersensitivity reactions, which may include anaphylaxis or angioedema Elevated liver enzymes Insomnia Depression Anxiety

Rare Common Adverse effects:

Anaphylaxis, a severe allergic reaction that can be life-threatening Hypersensitivity reactions, including drug rash with eosinophilia and systemic symptoms (DRESS) Malignancy, such as lymphoma Thrombosis, including deep vein thrombosis (DVT) and pulmonary embolism (PE)

The common side effects of Reslizumab include the following Injection site reactions (such as pain, redness, or swelling) Headache Fatigue Muscle pain Dizziness Itching.

Single doses of up to 732 mg have been administered intravenously to subjects in clinical trials without evidence of dose-related toxicities. There is no specific treatment for an overdose with reslizumab. If the event of an overdose, the patient should be treated supportively with appropriate monitoring as necessary.

Pharmacodynamic

Reslizumab an interleukin-5 (IL-5) antagonist (IgG4, kappa) that binds to IL-5 with a dissociation constant of 81 pM. IL-5 is a proinflammatory cytokine responsible for the terminal maturation of eosinophils and increases chemotaxis, endothelial adhesion, activation and survival of eosinophils. Eosinophils are known to play a central role in the pathophysiology of many patients with asthma; upon activation, eosinophils release leukotrienes, platelet activation factor, major basic protein, eosinophil cationic protein, eosinophil peroxidase, eosinophil-derived neurotoxin, and other cytokines that are cytotoxic to the bronchial epithelium and lead to airway inflammation and bronchospasm.

Pharmacokinetics

• Absorption: The peak serum concentrations of reslizumab were typically observed at the end of the infusion with the serum concentrations gradually declining from the peak in a biphasic manner. Following multiple doses, serum concentrations of reslizumab accumulated approximately 1.5 to 1.9-fold. Interindividual variability in peak and overall exposure across healthy individuals, patients with asthma, and other populations in pharmacokinetic studies was around 20-30% Label. Systemic exposure to reslizumab appeared to be unaffected by the presence of treatment-emergent anti-reslizumab antibodies.
• Distribution: The approximate volume of distribution of reslizumab is 5L, suggesting minimal distribution to the extravascular tissues
• Metabolism: Like other monoclonal antibodies, reslizumab is assumed to undergo enzymatic proteolysis into smaller peptides and amino acids. As reslizumab bind to the target, it is not expected to undergo a target-mediated clearance
• Excretion: Reslizumab clearance was approximately 7 mL/hour.

• https://www.rxlist.com/dopram-drug.htm
• https://www.mims.com/india/drug/info/Reslizumab ?type=full&mtype=generic
• https://go.drugbank.com/drugs/DB00561
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7003846/