PMID- 25505576
OWN - NLM
STAT- PubMed-not-MEDLINE
DCOM- 20141216
LR  - 20181113
IS  - 2052-1707 (Print)
IS  - 2052-1707 (Electronic)
IS  - 2052-1707 (Linking)
VI  - 2
IP  - 1
DP  - 2014 Feb
TI  - XG-102 administered to healthy male volunteers as a single intravenous infusion: 
      a randomized, double-blind, placebo-controlled, dose-escalating study.
PG  - e00020
LID - 10.1002/prp2.20 [doi]
LID - e00020
AB  - The aim of the study is to evaluate the safety, tolerability and pharmacokinetics 
      (PK) of the JNK inhibitor XG-102 in a randomized, double blind, placebo 
      controlled, sequential ascending dose parallel group Phase 1 Study. Three groups 
      of male subjects received as randomly assigned ascending single XG-102 doses (10, 
      40, and 80 mug/kg; 6 subjects per dose) or placebo (2 subjects per dose) as an 
      intravenous (IV) infusion over 60 min. Safety and tolerability were assessed by 
      physical examination, vital signs, electrocardiography, eye examination, clinical 
      laboratory tests and adverse events (AEs). PK was analyzed using noncompartmental 
      methods. All reported AEs were mild to moderate and neither their number nor 
      their distribution by System Organ Class suggest a dose relationship. Only 
      headache and fatigue were considered probably or possibly study drug related. 
      Headache frequency was similar for active and placebo, consequently this was not 
      considered to be drug related but probably to study conditions. The other 
      examinations did not show clinically relevant deviations or trends suggesting a 
      XG-102 relationship. Geometric mean half-life was similar among doses, ranging 
      from 0.36 to 0.65 h. Geometric mean XG-102 AUC0-last increased more than linearly 
      with dose, 90% confidence intervals (CIs) did not overlap for the two highest 
      doses. Geometric mean dose normalized C max values suggest a more than linear 
      increase with dose but 90% CIs overlap. It may be concluded that XG-102 single IV 
      doses of 10-80 mug/kg administered over 1 h to healthy male subjects were safe and 
      well tolerated.
FAU - Deloche, Catherine
AU  - Deloche C
AD  - Solid Drug Development Geneva, Switzerland.
FAU - Lopez-Lazaro, Luis
AU  - Lopez-Lazaro L
AD  - Covance Clinical Research Unit (CRU) Basel, Switzerland.
FAU - Mouz, Sebastien
AU  - Mouz S
AD  - Solid Drug Development Geneva, Switzerland.
FAU - Perino, Julien
AU  - Perino J
AD  - Solid Drug Development Geneva, Switzerland.
FAU - Abadie, Claire
AU  - Abadie C
AD  - Solid Drug Development Geneva, Switzerland.
FAU - Combette, Jean-Marc
AU  - Combette JM
AD  - Solid Drug Development Geneva, Switzerland.
LA  - eng
PT  - Journal Article
DEP - 20140126
PL  - United States
TA  - Pharmacol Res Perspect
JT  - Pharmacology research & perspectives
JID - 101626369
PMC - PMC4186400
OTO - NOTNLM
OT  - Clinical study
OT  - PK
OT  - XG-102
OT  - healthy volunteers
OT  - infusion
OT  - intravenous
OT  - phase I
OT  - safety
OT  - tolerability
EDAT- 2014/12/17 06:00
MHDA- 2014/12/17 06:01
PMCR- 2014/01/26
CRDT- 2014/12/16 06:00
PHST- 2013/07/29 00:00 [received]
PHST- 2013/11/14 00:00 [revised]
PHST- 2013/11/26 00:00 [accepted]
PHST- 2014/12/16 06:00 [entrez]
PHST- 2014/12/17 06:00 [pubmed]
PHST- 2014/12/17 06:01 [medline]
PHST- 2014/01/26 00:00 [pmc-release]
AID - 10.1002/prp2.20 [doi]
PST - ppublish
SO  - Pharmacol Res Perspect. 2014 Feb;2(1):e00020. doi: 10.1002/prp2.20. Epub 2014 Jan 
      26.