Cudarolimab

• CAT Number: I041532
• CAS Number: 2244739-29-3
• Purity: ≥95%

Cudarolimab (IBI101) is a completely human anti-OX40 (CD134, a co stimulating molecule expressed by activated immune cells) antibody. Cudarolimab inhibits the binding of OX40 to its ligand OX40L. Cudarolimab has antitumor activity and can be used in cancer related research[1].
Cudarolimab (0.01, 1, 100 or 10000 nM) binds to OX40 and partially blocks the binding of OX40 to its ligand OX40L in CHO-S cells overexpressing human OX40 (CHO-S-hOX40). Cudarolimab activates OX40 dependent NF-κB reporters with an EC50 value of 4.432 nM in Jurkat-OX40 reporter cells co-cultured with Raji cells[1].
Cudarolimab (0.01, 0.1, 1, 10, 100 or 1000 nM) binds to activated human CD4+ T cells and activated cynomolgus monkey CD4+ T cells in a dose dependent manner[1].
Cudarolimab (0.4, 4.0 and 40.4 nM) increases IL-2 secretion with dose dependent manner in human CD4+ T cells[1].
Cudarolimab (10 mg/kg; i.p.; single dose on days 3, 7, 11, 14 and 15) significantly reduces tumor volume in humanized NOG mice bearing LoVo tumors[1].
Cudarolimab (0.1, 1 and 10 mg/kg; i.p.; single dose on days 6, 9, 12 and 16) significantly reduces tumor volume, increases IFN-γ+ and IFN-α+ expression in CD8+ T cells in tumor and spleen of human OX40 knock-in mice bearing MC38 tumors[1].
Cudarolimab (10 mg/kg; i.p.; single dose on days 10 and 14) significantly reduces the expression of CD3+CD8+, CD3+CD4+, CD4+CD25highFoxP3+ in the tumor and spleen of human OX40 knock-in mice bearing MC38 tumors[1].
Pharmacokinetic (PK) parameters of Cudarolimab in cynomolgus macaques[1]

Dose (mg/kg)
Cmax (µg/mL )
Tmax (h)
AUC0-∞ (h•µg/mL )
T1/2 (h)
Cl (mL/h/kg)
MRTlast (h)

0.1
3.07±0.40
0.08±0.00
347.98±99.30
162.98±103.01
0.31±0.08
186.34±110.68

0.5
9.78±3.27
0.40±0.78
1429.19±607.21
129.47±114.44
0.40±0.14
136.03±108.05

2.5
63.10±15.29
0.08±0.00
10304.06±3403.59
190.89±92.94
0.27±0.09
212.29±114.61

12.5
296.57±58.05
0.40±0.78
33511.65±14982.36
120.30±153.26
0.44±0.20
114.93±87.66

Reference

[1]. Kuang Z, et al. Development and characterization of a novel anti-OX40 antibody for potent immune activation. Cancer Immunol Immunother. 2020 Jun;69(6):939-950.
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