Research
Title : | Finding Novel Cost-effective Process and Formulation of RISDIPLAM to treat Spinal muscular atrophy SMA |
Area of Research : | Pharmaceutical Sciences |
Focus Area : | Formulation Science |
Principal Investigator : | Dr. H Yogish Kumar, JSS College of Pharmacy, Mysuru, Karnataka (570015) |
Co-PI: | Dr. Akila Prashant, JSS Medical College, Mysuru, Karnataka (570015), Dr. Balamuralidhara V, JSS College of Pharmacy, Mysuru, Karnataka (570015), Dr. Mahagundappa R Maddani, Mangalore University, Mangalore Karnataka (574199), Dr. Nemichandra S C, Jss Medical College, Mysuru, Karnataka (570015), Dr. Osmani Mir Riyaz Ali Mahafez Ali, Jss College of Pharmacy, Mysuru, Karnataka (570015), Dr. Saravana Babu C, JSS College of Pharmacy, Mysuru, Karnataka (570015) |
Contact info : | hyogishkumar@jssuni.edu.in; akilaprashant@jssuni.edu.in; baligowda@jssuni.edu.in; mahagundappa@mangaloreuniversity.ac.in; nemichandra85@gmail.com; riyazosmani@jssuni.edu.in; saravanababu.c@jssuni.edu.in |
Total Budget (INR): | 39,99,000 |
Details
Executive Summary : | The primary objective is to develop a cost-effective non-fringing synthetic route of Risdiplam, enhancing its efficacy and pharmacokinetic parameters. The RISDIPLAM synthesis is planned through a convergent process, involving the synthesis of Compound A B and coupling of Compound A B2 using a Pd-based catalyst. The synthesis of Compound A involves the aromatic nucleophilic substitution Boc-4,7-diazaspiro[2.5]octane with p-bromonitropyridine, which is reduced using a catalyst other than Rn-Ni/Pd-C. Compound D is cyclized using methyl dimethylmalonate in the presence of a suitable amphiphilic catalyst, yielding compound B. Compound A1 is synthesized by converting ethylacetoacetate to B1 in the presence of a non-nucleophilic base, which is then halogenated to yield compound A. Compound B2 is subsequently prepared using a bispinacolatodiborane pd catalyst. The drug formulation will be developed using a novel nanotechnology-based strategy using ultrasonication crystallization technique. The validation of the synthesized drug compound will be tested using cell-based assays to understand its ability to increase SMN protein levels. The development of a novel route of synthesis and formulation will reduce the cost of drug substance and formulation, ultimately reducing the burden on Indian populations, particularly infants and young children. |
Equipments : | Magnetic stirrer with hot ( Rs.150500.00 ) , Magnetic stirrer with hot ( Rs.0.00 ) , Overhea d stirrer/ Laborato ry stirrer ( Rs.33500.00 ) , Overhea d stirrer/ Laborato ry stirrer ( Rs.0.00 ) , Weighing Balance ( Rs.105500.00 ) , Weighing Balance ( Rs.0.00 ) , Heating mantle ( Rs.14500.00 ) , Heating mantle ( Rs.0.00 ) |
Organizations involved
Implementing Agency : | JSS College of Pharmacy, Mysuru, Karnataka Funding Agency :Department of Science and Technology (DST) | Source:Department of Science and Technology (DST) | |