Table 1.
PTP inhibitors that have been evaluated in vivo
Inhibitor | PTP | Animal Studies | Human Trials | Firm | Reference |
---|---|---|---|---|---|
BN82002 Cmp 26* |
Cdc25 | Inhibit Mia PaCa-2 pancreatic tumor xenograft growth. |
IPSEN | [156] | |
BN82685 Cmp 27 |
Cdc25 | Inhibit Mia PaCa-2 pancreatic tumor xenograft growth. |
IPSEN | [157] | |
IRC-083864 Debio-0931 Cmp 25 |
Cdc25 | Inhibit Mia PaCa-2 pancreatic tumor and LNCaP prostate tumor xenograft growth. |
Phase I (planned) | IPSEN/ Debiopharm |
[155] |
Cmp 17 | PTP1B | Lower blood glucose level. Delay onset of ErbB2-induced mammary tumor. |
Merck Frosst | [102] | |
Ertiprotafib Cmp 18 |
PTP1B | Lower fasting blood glucose and insulin. Improve glycemic excursion. Improve lipid profiles. |
Phase II in type II diabetes (Discontinued because of insufficient efficacy and concerns about side-effects due to inhibition of other targets) |
Wyeth Research |
[107] |
MSI-1436 Trodusquemine Cmp 19 |
PTP1B | Suppress appetite Induce fat-specific weight loss Improve insulin and leptin levels |
Phase I | Genaera | [108] |
Cmp 13 | Glepp1 | Inhibit thioglycolate-induced peritonitis. Inhibit dermatitis. Inhibit ulcerative colitis. |
Merck Serono |
[90] |
Cmp: compound