Last reviewed 2026-04-23 · How we verify

Ruboxistaurin mesylate

Ruboxistaurin mesylate is a protein kinase C (PKC) beta inhibitor that reduces vascular permeability and inflammation in diabetic microvascular complications.

Ruboxistaurin mesylate is a protein kinase C (PKC) beta inhibitor that reduces vascular permeability and inflammation in diabetic microvascular complications. Used for Diabetic macular edema (DME), Diabetic retinopathy.

At a glance

Mechanism of action

The drug selectively inhibits PKC-beta, an enzyme overactivated in hyperglycemic conditions that drives pathological changes in blood vessels. By blocking PKC-beta signaling, ruboxistaurin reduces vascular permeability, inflammation, and abnormal cell growth in the retina and kidney, thereby slowing progression of diabetic retinopathy and nephropathy.

Approved indications

• Diabetic macular edema (DME)
• Diabetic retinopathy

Common side effects

• Headache
• Dizziness
• Gastrointestinal disturbances
• Hyperglycemia

Key clinical trials

• Treatment for Symptomatic Peripheral Neuropathy in Patients With Diabetes (PHASE3)
• The Effect of Ruboxistaurin on Small Fiber Function (PHASE2)
• Treatment for Symptomatic Peripheral Neuropathy in Patients With Diabetes (PHASE3)
• Treatment of Peripheral Neuropathy in Patients With Diabetes (PHASE3)

Primary sources

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Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Ruboxistaurin mesylate CI brief — competitive landscape report
• Ruboxistaurin mesylate updates RSS · CI watch RSS
• Chromaderm, Inc. portfolio CI