The antiherpetic effects of 9-(1,3-dihydroxy-2-propoxymethyl)guanine (DHPG) in vitro and in vivo were investigated in comparison with those of acyclovir (ACV) and 5-iodo-2'-deoxyuridine (IDU). ACV was found to be consistently superior to the other two agents in antiviral activity against all ocular isolates in vitro. In vivo tests in mice, in contrast, showed DHPG in ointment form to be more effective than ACV in treating herpetic keratitis. It was noted that even 0.03% DHPG ointment was as efficacious as 0.3% ACV ointment. Other studies using the same keratitis model also demonstrated that DHPG eyedrop solution is far more effective than IDU eyedrop solution. These results indicate that DHPG can be a useful antiviral agent in the treatment of herpetic keratitis.