Elimusertib shows potent anti-tumor efficacy in monotherapy in a variety of xenograft models of ovarian and colorectal cancer, and causes complete tumor remission in mantle cell lymphoma models[2].
Elimusertib (50 mg/kg; p.o.; b.i.d.; 3 days on/4 days off; for 11 days) exhibits strong antitumor efficacy in the ATM-mutated SU-DHL-8 (ATM K1964E) human GCB-DLBCL cell line derived xenograft model in mice[3].
Elimusertib (20 mg/kg, and 10 mg/kg from day 14; p.o.; daily; 2 days on/5 days off; for 42 days) in combination with Carboplatin (40 mg/kg; i.p.; daily; 1 day on/6 days off) results in synergistic antitumor activity in the platinum-resistant ATM protein low expressing CR5038 human CRC PDX model in NOD/SCID mice[3].
Elimusertib exhibits moderate oral bioavailability (rat 87%, dog 51%) following oral administration (rat and dog 0.6-1 mg/kg)[3].
Elimusertib exhibits terminal elimination half-lives (mouse 0.17 h, rat 1.3 and, dog 1.0 h) due to plasma clearance (3.5, 1.2, and 0.79 L/h/kg respectively) following intravenous administration (mouse, rat and dog 0.3-0.5 mg/kg)[3].
| Animal Model: | Female C.B-17 SCID mice, SU-DHL-8 GCB-DLBCL xenograft model[3] |
| Dosage: | 50 mg/kg |
| Administration: | Oral administration, b.i.d., 3 days on/4 days off, for 11 days |
| Result: | Inhibited tumor area. |
| Animal Model: | Male Wistar rats[3] |
| Dosage: | 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral administration |
| Result: | Oral bioavailability (87%), T1/2 (1.3 h). |
| Animal Model: | Female beagle dogs[3] |
| Dosage: | 0.3-0.5 mg/kg for i.v.; 0.6-1 mg/kg for oral (Pharmacokinetic Analysis) |
| Administration: | Intravenous injection and oral administration |
| Result: | Oral bioavailability (51%), T1/2 (1.0 h). |
