Phase 1 Study of CEP-37250/KHK2804, a Tumor-Specific Anti-Glycoconjugate Monoclonal Antibody

Phase 1 Study of CEP-37250/KHK2804, a Tumor-specific Anti-glycoconjugate Monoclonal Antibody, in Patients with Advanced Solid Tumors

Monica M. Mita, John Nemunaitis, Juneko Grilley-Olson, Bassil El-Rayes, Tanios Bekaii-Saab, R. Donald Harvey, John Marshall, Xiaoping Zhang, Vincent StroutMonica M. Mita1*, Vincent Strout2

Supplementary Table S1 Pharmacokinetics of CEP-37250/KHK2804 after once weekly IV administration during cycle 1 to patients with advanced solid tumors during dose escalation in phase 1a

CEP-37250/KHK2804 dose / Day / No. of patients / Mean±SD
Tmax
(h) / Cmax
(ng/ml) / AUC0–t
(µg•h/ml) / AUC0–∞
(µg•h/ml) / t1/2
(h)
0.03 mg/kg / 1 / 7 / 2.20±0.850 / 714±339 / 26.7±20.5 / 41.8±37.0 / 49.2±27.1
22 / 6 / 2.90±1.16 / 857±555 / 49.2±43.5 / – / 70.3±28.6a
0.01 mg/kg / 1 / 6 / 2.71±0.307 / 2,120±713 / 64.6±26.6 / 77.9±35.0 / 34.1±13.0
22 / 5 / 4.40±2.09 / 3,880±2,030 / 112±48.6 / – / 38.1±18.2
0.3 mg/kg / 1 / 7 / 4.36±2.25b / 6,760±3,509 / 289±224 / 430±382 / 44.3±28.8
22 / 5 / 2.85±0.792 / 14,600±16,100 / 666±744 / – / 67.0±56.5c
1 mg/kg / 1 / 7 / 4.05±0.479d / 19,200±2,730d / 746±207 / 949±403 / 41.9±28.8
22 / 4 / 3.99±1.67 / 25,100±16,900 / 1,110±844 / – / 44.6±24.7d

AUC0–t, area under the serum concentration-time curve from time zero to the time of the last measurable concentration; AUC0–∞, area under the serum concentration-time curve from time zero to infinity; Cmax, maximum serum concentration; SD, standard deviation; Tmax, time to Cmax; t1/2, elimination half-life

a n=5

b n=6

c n=4

d n=3

Supplementary Table S2 Pharmacokinetics of CEP-37250/KHK2804 after once weekly IV administration 0.3 mg/kg during cycle 1 to patients in patients with advanced colorectal and pancreatic cancer during dose expansion in phase 1b

Cohort / Day / No. of patients / Mean±SD
Tmax
(h) / Cmax
(ng/mL) / AUC0–t
(µg•h/ml) / AUC0–∞
(µg•h/ml) / t1/2
(h)
Colorectal / 1 / 15 / 3.67±2.0a / 8240±4840 / 201±180 / 307±295 / 49.4±40.6
22 / 6 / 2.71±0.878b / 7570±6020 / 289±277 / – / 72.8±29.2
Pancreatic / 1 / 13 / 3.32±1.31c / 4790±2590c / 289±277 / 160±180d / 39.4±18.9d
22 / 8 / 2.94±1.14 / 7170±4630 / 288±283 / – / 58.6±50.0

AUC0–t, area under the serum concentration-time curve from time zero to the time of the last measurable concentration; AUC0–∞, area under the serum concentration-time curve from time zero to infinity; Cmax, maximum serum concentration; SD, standard deviation; Tmax, time to Cmax; t1/2, elimination half-life

a n=9

b n=5

c n=8

d n=12