Comparison of the ocular hypotensive lipid AGN 192024 with timolol: dosing, efficacy, and safety evaluation of a novel compound for glaucoma management.
OBJECTIVE
To compare the safety and efficacy of the ocular hypotensive lipid AGN 192024 (Lumigan) with those of timolol.


METHODS
A 30-day, randomized, investigator-masked, clinical trial involving 100 patients with elevated intraocular pressure (IOP). Study medications were instilled topically. Doses of 0.003%, 0.01%, or 0.03% AGN 192024 were given once daily for 3 weeks then twice daily for 1 week, and vehicle control or 0.5% timolol was given twice daily for 4 weeks. Mean change in IOP from baseline was the primary efficacy variable. Safety parameters included adverse events, hyperemia grading, laser flare meter analysis, heart rate, and blood pressure.


RESULTS
Timolol and all 3 concentrations of AGN 192024 lowered IOP from baseline (P < .001). A dosage of 0.03% AGN 192024 once daily lowered IOP significantly more than timolol (P < or = .02) at every study visit except day 21 (P = .053) and provided better diurnal IOP control. Twice-daily dosing of AGN 192024 provided no clinically significant benefit over once-daily dosing. All treatment regimens were safe and well tolerated, with no clinically significant effects on heart rate or blood pressure and no between-group differences in the incidence of adverse events. The only significant ocular safety finding with AGN 192024 was a dose-related mild increase in conjunctival hyperemia.


CONCLUSIONS
Of the 3 concentrations tested, 0.03% AGN 192024 once daily had the best therapeutic profile. AGN 192024 was safe and well tolerated, and it provided superior ocular hypotensive efficacy and diurnal IOP control compared with timolol in patients with ocular hypertension and glaucoma.
Laibovitz
R A
RA
Eye Research Associates, Austin TX, USA.
VanDenburgh
A M
AM
Felix
C
C
David
R
R
Batoosingh
A
A
Rosenthal
A
A
Cheetham
J
J
D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000577:Amides; D000959:Antihypertensive Agents / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D000069580:Bimatoprost; D002940:Circadian Rhythm; D003008:Cloprostenol / Q000031:analogs & derivatives; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004341:Drug Evaluation; D005260:Female; D006439:Hemodynamics; D006801:Humans; D007429:Intraocular Pressure / Q000187:drug effects*; D008055:Lipids / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D009798:Ocular Hypertension / Q000188:drug therapy*; D009883:Ophthalmic Solutions; D012449:Safety; D013999:Timolol / Q000008:administration & dosage* / Q000009:adverse effects / Q000627:therapeutic use
D000577:Amides; D000959:Antihypertensive Agents; D008055:Lipids; D009883:Ophthalmic Solutions; D003008:Cloprostenol; D013999:Timolol; D000069580:Bimatoprost