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reslizumab

Product Namereslizumab
CAS241473-69-8
MF
MW0
EINECS
MOL FileMol File

Chemical Properties

storage temp.	Store at 4°C,Do not freeze
solubility	Soluble in DMSO
form	Liquid
color	Colorless to light yellow

Usage And Synthesis

Uses

Reslizumab (Sch 55700) is humanized monoclonal antibodies that target interleukin-5 (IL-5) for the treatment of eosinophilic asthma. Reslizumab is effective in neutralizing the function of IL-5. Reslizumab has high binding affinity for human IL-5, with KD values of 109 pM and 4.3 pM in the the Biacore surface plasmon resonance and Kinetic Exclusion Assay, respectively[1][2].

Clinical Use

Treatment of severe eosinophilic asthma

in vivo

Reslizumab (Sch 55700) (0-10 mg/kg; i.p. or i.m.) inhibits pulmonary eosinophilia in a dose-dependent manner in allergic mice^[3].
Reslizumab (0.03-30 mg/kg; i.p.) inhibits both the pulmonary eosinophilia and airway hyperresponsiveness, and at 30 mg/kg, i.p. inhibits allergic, but not histamine-induced bronchoconstriction in allergic guinea pigs^[3].
Reslizumab (0.1-1 mg/kg; i.p.) blocks the pulmonary eosinophilia and neutrophilia caused by tracheal injection of hIL-5 in guinea pigs^[3].
Reslizumab (0.3 mg/kg; i.v.) blocks the pulmonary eosinophilia caused by antigen challenge for up to six months in allergic cynomolgus monkeys^[3].

Animal Model:	Male B6D2F1/J mice weighing 2025 g, sensitized by an intraperitoneal injection of 0.5 ml of alum-precipitated antigen (8 μg of ovalbumin (OVA) adsorbed to 2 mg of aluminum hydroxide gel in saline vehicle)^[3]
Dosage:	010 mg/kg
Administration:	Intraperitoneal or intramuscular injection (For studies involving i.p. dose-response and i.m. evaluation, the antibody was given 2 h before OVA challenge. For experiments involving duration of activity, the antibody was given at times of 2 h or 4, 6, 8 or 12 weeks before antigen challenge.)
Result:	Inhibited the influx of eosinophils into the lungs for a long time (up to 8 weeks after administration of 10 mg/kg and for up to 4 weeks after administration of 2 mg/kg. Demonstrated an anti-inflammatory activity that was additive to that of oral Prednisolone (HY-17463).

Drug interactions

Potentially hazardous interactions with other drugs
Vaccines: risk of generalised infections with live vaccines - avoid.

IC 50

IL-5: 91.1 pM (IC₅₀)

Metabolism

Reslizumab is believed to be degraded by enzymatic proteolysis into small peptides and amino acids. As reslizumab binds to a soluble target, linear non-targetmediated clearance is expected.

References

[1] Liddament M, et al. Higher Binding Affinity and in vitro Potency of Reslizumab for Interleukin-5 Compared With Mepolizumab. Allergy Asthma Immunol Res. 2019 Mar;11(2):291-298. DOI:10.4168/aair.2019.11.2.291
[2] Pérez de Llano LA, et al. Mepolizumab and reslizumab, two different options for severe asthma patients with prior failure to omalizumab. Allergy. 2019 Sep 4. DOI:10.1111/all.14035
[3] Egan RW, Effect of Sch 55700, a humanized monoclonal antibody to human interleukin-5, on eosinophilic responses and bronchial hyperreactivity. Arzneimittelforschung. 1999 Sep;49(9):779-90. DOI:10.1055/s-0031-1300502

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