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Table 1 Summary of eleven first-in-human drugs presented at this year's ASCO meeting.

From: First-in-class, first-in-human phase I results of targeted agents: Highlights of the 2008 American Society of Clinical Oncology 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
  1. †Clinical efficacy was not available at time of presentation for all patients enrolled in these studies, therefore these response rates do not represent the whole study cohort and may change in the future
  2. Abbreviations: TBD – to be determined; MTD – maximum tolerated dose; RPTD – recommended phase II dose; CR – complete response; PR – partial response; SD – stable disease; i.v. – intravenous; Misc – miscellaneous; NHL – non-Hodgkin's lymphoma; GBM – gliobastome multiforme; PTT – partial thromboplastin time; s.c. – deep subcutaneous; GI – gastrointestinal (including all 3 of nausea/vomiting/diarrhea); BCC – basal cell carcinoma; RPLS – Reversible posterior leucoencephalopathy syndrome