Trioxanes are the new antimalarial series of potent compound having the capability to harness the over growing menace of malaria and its acquisition of resistance. In this manuscript the authors have presented results of the metabolic studies of a potent trioxane series of antimalarial compound, CDRI-97/78, developed at Central Drug Research Institute. About 75% of the CDRI-97/78 was metabolised to CDRI-97/63. Further metabolites of CDRI-97/63 were not noticed. The metabolism of CDRI compound 97/78 and 97/63 was mainly in the microsomal fraction only a small fraction can be attributed towards the cytosolic fraction, thus reflecting the prominence of Phase 1 reactions during metabolism. The metabolic reaction as depicted by the kinetic parameters show that the clearance of CDRI- 97/78 is about twice more in S9 fraction as compared to the microsomal fraction. Thus pointing towards further metabolism of the CDRI- 97/63, also the nonsignificant change observed in case of the Vmax and velocity in S9 and microsomal fraction depict the that majorily one isoform of cytochrome P-450 is involved in the metabolism of CDRI-97/78. Ketoconazole (CYP3A2 inhibitor) and Aminobenzotriazole completely inhibited the rate of reaction depicting the involvement of Phase 1 reactions particularly CYTOCHROME P450 3A2 isoform; whereas, verapamil (CYP2E1); cimetidine (CYP1A2); omeprazole (CYP2C19); quinidine (CYP2D6); sulphaphenazole and isoniazid (CYP2C9) did not affected the rate of reaction.