Table 1 Summary of eleven first-in-human drugs presented at this year's ASCO meeting.
Drug name | Target | Route | Tumor sites enrolled | Common low-grade adverse effects | Dose-limiting toxicities | RPTD | Clinical efficacy | Phase II studies planned/o pen |
|---|---|---|---|---|---|---|---|---|
BMS-663513 | CD-137 agonist | i.v. | Melanoma Renal cell Ovarian | Fatigue Rash/pruritis Diarrhea Fever | Neutropenia Transaminitis | TBD (range from 0.1–5 mg/kg every 3 weeks) | 6% PR 15% SD†| Melanoma |
CT-322 | VEGFR-2 | i.v. | Misc. solid tumors and NHL | Proteinuria Hypertension | Proteinuria RPLS Retinal vascular occlusion | MTD of 2 mg/kg/week, RPTD not specified | 49% SD†| GBM |
CVX-045 | Thrombospondin | i.v. | Misc. solid tumors | Fatigue GI Dyspnea Headache Dizziness | None 1 radiation pneumonitis 1 death (bowel obstruction) | 12 mg/kg/week | 5% PR 33% SD | TBD |
GDC-0449 | Smoothened | oral | Misc. solid tumors | Dysguesia Hyponatremia Fatigue | None | 150 mg daily | 11% PR 11% SD | Colorectal Ovarian BCC |
GRN163L | Telomerase | i.v. | Misc. solid tumors | Prolonged PTT GI Fatigue | Thrombocytopenia One death (unknown cause) | TBD | TBD | TBD |
LY2181308 | Survivin | i.v. | Misc. solid tumors | Fever Fatigue Prolonged PTT Nausea | Headache | 750 mg daily for 3 days, then weekly | 10% SD | Prostate |
PF-00562271 | FAK | oral | Misc. solid tumors | GI Headache Fatigue Dizziness | Headache Nausea | 125 mg twice daily | 17% SD | TBD |
RAV12 | RAAG12 | i.v. | GI cancers | Diarrhea Abdominal discomfort Transaminitis | Diarrhea Abdominal discomfort Transaminitis | 0.75 mg/kg twice weekly | 2% PR 20% SD†| Pancreas Colorectal |
RTA 402 | NF-κB and STAT3 | oral | Misc. solid tumors and NHL | GI Fatigue Anorexia Dysguesia | ALT elevation | 900 mg/day | 7% CR + PR 40% SD†| Pancreas Melanoma |
XL765 | PI3K and mTOR | oral | Misc. solid tumors | Transaminitis Diarrhea Anorexia Fatigue | Transaminitis Diarrhea | Possibly 60 mg twice daily | 26% SD | TBD |
Survivin vaccine | Survivin | s.c. | Melanoma | Injection site reactions Fever Lymph node swelling | None | TBD | 8% CR+PR | TBD |