For the growth and spread of a tumor beyond 2 mm, angiogenesis plays a crucial role, and association of various integrins with angiogenesis is evidential. The aim of the study was radiolabeling of DOTA-chelated RGD (arginine-glycine-aspartic acid) peptide with ⁶⁸Ga for PET imaging in locally advanced breast carcinoma. DOTA-RGD was incubated with ⁶⁸GaCl₃, eluted in 0.05m HCl. Elution volume, peptide amount, and reaction pH were studied. Radio-ITLC, gas chromatography, endotoxin, and sterility testing were performed. Serial (n = 3) and whole-body (n = 2) PET/CT imaging was done on patients post i.v. injection of 111–185MBq of ⁶⁸Ga-DOTA-RGD. Maximum radiolabeling yield was achieved with 3mL elution volume of 15–20 µg peptide at pH 3.5–4.0 with 10 minutes of incubation at 95°C. Product samples were sterile having 99.5% radiochemical purity with residual ethanol content and endotoxins in injectable limits. Intense radiotracer uptake was noticed in the tumor with SUV_max 15.3 at 45 minutes in serial images. Physiological radiotracer uptake was seen in the liver, spleen, ventricles, and thyroid with excretion through the kidneys. The authors concluded that ⁶⁸Ga-DOTA-RGD has the potential for imaging α,vβ₃ integrin-expressing tumors.