GR122311X (ranitidine bismuth citrate), a new drug for the treatment of duodenal ulcer.
BACKGROUND
Ranitidine bismuth citrate (GR122311X) is a new drug which offers potential benefits in healing duodenal ulcers and prevention of relapse.


METHODS
This randomized, multi-centre double-blind study of 1620 patients compared the effect of 4 weeks of treatment with GR122311X 200 mg b.d. (n = 401), 400 mg b.d. (n = 404) or 800 mg b.d. (n = 404) or ranitidine hydrochloride 150 mg b.d. (n = 411) on the rates of duodenal ulcer healing and of overall success (ulcers healed and remaining ulcer free in the 24-week follow-up phase).


RESULTS
All four treatments were equally effective at ulcer healing (79%, 85%, 84% and 81% of patients, respectively). GR122311X 400 mg b.d. (38%) and 800 mg b.d. (37%) were significantly more effective than ranitidine hydrochloride 150 mg b.d. (32%) with respect to overall success (P = 0.050 and P = 0.030, respectively) but there was no difference with GR122311X 200 mg b.d. (31%). GR122311X caused effective, dose-related suppression of H. pylori (47%, 61% and 74%); H. pylori eradication rates were 18%, 21% and 22%. GR122311X was safe and well tolerated, with an adverse event profile similar to that of ranitidine hydrochloride 150 mg b.d. Median week 4 trough plasma bismuth levels were 1.3 ng/mL, 2.3 ng/mL and 3.3 ng/mL with GR122311X 200 mg b.d., 400 mg b.d. and 800 mg b.d. respectively. No individual plasma bismuth concentrations were of clinical concern.


CONCLUSIONS
GR122311X is a safe and effective ulcer healing drug, and provides a platform on which anti-H. pylori therapy can be based.
Bardhan
K D
KD
Rotherham General Hospitals NHS Trust, UK.
Dekkers
C P
CP
Lam
S K
SK
Nowak
A
A
Schaffalitzky de Muckadell
O B
OB
Schutze
K
K
Tildesley
G
G
Kler
L
L
Forster
J K
JK
Lacey
L F
LF
D000328:Adult; D001729:Bismuth / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004381:Duodenal Ulcer / Q000097:blood / Q000188:drug therapy* / Q000382:microbiology; D005260:Female; D016481:Helicobacter Infections / Q000188:drug therapy / Q000382:microbiology; D016480:Helicobacter pylori / Q000187:drug effects; D006635:Histamine H2 Antagonists / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D006801:Humans; D016015:Logistic Models; D008297:Male; D008875:Middle Aged; D011899:Ranitidine / Q000008:administration & dosage / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000627:therapeutic use; D016896:Treatment Outcome
D006635:Histamine H2 Antagonists; C073340:ranitidine bismuth citrate; D011899:Ranitidine; D001729:Bismuth