Immunosuppressants & Transplant Care

Azathioprine Tablets (50 mg) is an oral imidazolyl derivative prodrug of 6-mercaptopurine (6-MP) on the WHO Model List of Essential Medicines. It is non-enzymatically cleaved by glutathione into 6-MP, which is intracellularly converted to 6-thioguanine nucleotides (6-TGN). 6-TGN incorporates into replicating DNA, causing chain termination, and inhibits de novo purine synthesis, suppressing clonal expansion of T- and B-lymphocytes. Indicated as an adjunct for prevention of rejection in renal allotransplantation and severe rheumatoid arthritis, lupus nephritis, Crohn's disease, ulcerative colitis, and autoimmune hepatitis.

Cyclosporine / Cyclosporin Capsules (25mg, 50mg, 100mg) is a cyclic polypeptide calcineurin inhibitor on the WHO Model List of Essential Medicines. Inside T-helper lymphocytes, it binds to the immunophilin cyclophilin; the resulting complex inhibits calcineurin phosphatase, preventing the dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NF-AT). This completely suppresses transcription of interleukin-2 (IL-2) and subsequent T-cell activation and proliferation. Indicated for prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants, and severe rheumatoid arthritis, psoriasis, and nephrotic syndrome.

Mycophenolate Mofetil Tablets (500mg) and Mycophenolate Sodium Gastro-Resistant Tablets (360mg) is an oral prodrug of mycophenolic acid (MPA) on the WHO Model List of Essential Medicines. MPA is a potent, selective, non-competitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), the rate-limiting enzyme in de novo guanine nucleotide synthesis. Because T- and B-lymphocytes rely almost exclusively on the de novo pathway for purine generation (unlike other cell types that utilize the salvage pathway), mycophenolate selectively blocks lymphocyte proliferation and antibody production. Indicated in combination with cyclosporine/tacrolimus and corticosteroids for prophylaxis of organ rejection in kidney, heart, and liver allografts, and for induction and maintenance of lupus nephritis.

Cyclosporine / Cyclosporin Capsules (25mg, 50mg, 100mg) is a cyclic polypeptide calcineurin inhibitor on the WHO Model List of Essential Medicines. Inside T-helper lymphocytes, it binds to the immunophilin cyclophilin; the resulting complex inhibits calcineurin phosphatase, preventing the dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NF-AT). This completely suppresses transcription of interleukin-2 (IL-2) and subsequent T-cell activation and proliferation. Indicated for prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants, and severe rheumatoid arthritis, psoriasis, and nephrotic syndrome.

Cyclosporine / Cyclosporin Capsules (25mg, 50mg, 100mg) is a cyclic polypeptide calcineurin inhibitor on the WHO Model List of Essential Medicines. Inside T-helper lymphocytes, it binds to the immunophilin cyclophilin; the resulting complex inhibits calcineurin phosphatase, preventing the dephosphorylation and nuclear translocation of nuclear factor of activated T-cells (NF-AT). This completely suppresses transcription of interleukin-2 (IL-2) and subsequent T-cell activation and proliferation. Indicated for prophylaxis of organ rejection in kidney, liver, and heart allogeneic transplants, and severe rheumatoid arthritis, psoriasis, and nephrotic syndrome.

Tacrolimus Capsules (0.25mg, 1mg, 2mg) is a potent macrolide calcineurin inhibitor on the WHO Model List of Essential Medicines. It binds to intracellular FK506-binding protein-12 (FKBP-12); the drug-protein complex binds and inhibits calcineurin phosphatase with 10- to 100-fold higher potency than cyclosporine, extinguishing IL-2 gene transcription, T-cell proliferation, and cytotoxic lymphocyte generation. Indicated for prophylaxis of organ rejection in patients receiving allogeneic kidney, liver, or heart transplants, and rescue therapy in refractory rejection.

Tacrolimus Capsules (0.25mg, 1mg, 2mg) is a potent macrolide calcineurin inhibitor on the WHO Model List of Essential Medicines. It binds to intracellular FK506-binding protein-12 (FKBP-12); the drug-protein complex binds and inhibits calcineurin phosphatase with 10- to 100-fold higher potency than cyclosporine, extinguishing IL-2 gene transcription, T-cell proliferation, and cytotoxic lymphocyte generation. Indicated for prophylaxis of organ rejection in patients receiving allogeneic kidney, liver, or heart transplants, and rescue therapy in refractory rejection.

Tacrolimus Capsules (0.25mg, 1mg, 2mg) is a potent macrolide calcineurin inhibitor on the WHO Model List of Essential Medicines. It binds to intracellular FK506-binding protein-12 (FKBP-12); the drug-protein complex binds and inhibits calcineurin phosphatase with 10- to 100-fold higher potency than cyclosporine, extinguishing IL-2 gene transcription, T-cell proliferation, and cytotoxic lymphocyte generation. Indicated for prophylaxis of organ rejection in patients receiving allogeneic kidney, liver, or heart transplants, and rescue therapy in refractory rejection.

Mycophenolate Mofetil Tablets (500mg) and Mycophenolate Sodium Gastro-Resistant Tablets (360mg) is an oral prodrug of mycophenolic acid (MPA) on the WHO Model List of Essential Medicines. MPA is a potent, selective, non-competitive, and reversible inhibitor of inosine monophosphate dehydrogenase (IMPDH), the rate-limiting enzyme in de novo guanine nucleotide synthesis. Because T- and B-lymphocytes rely almost exclusively on the de novo pathway for purine generation (unlike other cell types that utilize the salvage pathway), mycophenolate selectively blocks lymphocyte proliferation and antibody production. Indicated in combination with cyclosporine/tacrolimus and corticosteroids for prophylaxis of organ rejection in kidney, heart, and liver allografts, and for induction and maintenance of lupus nephritis.

Sirolimus / Rapamycin Tablets (1mg) is a macrocyclic lactone immunosuppressive agent on the WHO Model List framework. It binds intracellularly to immunophilin FKBP-12, but unlike tacrolimus, the sirolimus-FKBP-12 complex binds to and inhibits the mammalian target of rapamycin (mTOR) kinase complex 1 (mTORC1). This blocks IL-2-stimulated progression from G1 to S phase in T-lymphocytes. Completely non-nephrotoxic compared to calcineurin inhibitors. Indicated for prophylaxis of organ rejection in kidney transplant recipients (often to spare calcineurin inhibitor nephrotoxicity) and treatment of lymphangioleiomyomatosis (LAM).

Everolimus Tablets (0.25mg, 0.5mg, 5mg, 10mg) is an oral derivative of rapamycin that selectively inhibits the mTORC1 serine/threonine kinase complex on the WHO Model List of Essential Medicines. In oncology, mTOR inhibition halts downstream protein synthesis (p70S6K, 4E-BP1), blocking cell proliferation, nutrient sensing, and VEGF-driven angiogenesis. In organ transplantation, it suppresses lymphocyte activation. Indicated for HR+/HER2- advanced breast cancer (with exemestane), advanced renal cell carcinoma, pancreatic/gastrointestinal/lung neuroendocrine tumors (NET), subependymal giant cell astrocytoma (SEGA), and renal angiomyolipoma with tuberous sclerosis; lower doses (0.25/0.5mg) are used for kidney and liver transplant rejection prophylaxis.

Everolimus Tablets (0.25mg, 0.5mg, 5mg, 10mg) is an oral derivative of rapamycin that selectively inhibits the mTORC1 serine/threonine kinase complex on the WHO Model List of Essential Medicines. In oncology, mTOR inhibition halts downstream protein synthesis (p70S6K, 4E-BP1), blocking cell proliferation, nutrient sensing, and VEGF-driven angiogenesis. In organ transplantation, it suppresses lymphocyte activation. Indicated for HR+/HER2- advanced breast cancer (with exemestane), advanced renal cell carcinoma, pancreatic/gastrointestinal/lung neuroendocrine tumors (NET), subependymal giant cell astrocytoma (SEGA), and renal angiomyolipoma with tuberous sclerosis; lower doses (0.25/0.5mg) are used for kidney and liver transplant rejection prophylaxis.

Everolimus Tablets (0.25mg, 0.5mg, 5mg, 10mg) is an oral derivative of rapamycin that selectively inhibits the mTORC1 serine/threonine kinase complex on the WHO Model List of Essential Medicines. In oncology, mTOR inhibition halts downstream protein synthesis (p70S6K, 4E-BP1), blocking cell proliferation, nutrient sensing, and VEGF-driven angiogenesis. In organ transplantation, it suppresses lymphocyte activation. Indicated for HR+/HER2- advanced breast cancer (with exemestane), advanced renal cell carcinoma, pancreatic/gastrointestinal/lung neuroendocrine tumors (NET), subependymal giant cell astrocytoma (SEGA), and renal angiomyolipoma with tuberous sclerosis; lower doses (0.25/0.5mg) are used for kidney and liver transplant rejection prophylaxis.

Everolimus Tablets (0.25mg, 0.5mg, 5mg, 10mg) is an oral derivative of rapamycin that selectively inhibits the mTORC1 serine/threonine kinase complex on the WHO Model List of Essential Medicines. In oncology, mTOR inhibition halts downstream protein synthesis (p70S6K, 4E-BP1), blocking cell proliferation, nutrient sensing, and VEGF-driven angiogenesis. In organ transplantation, it suppresses lymphocyte activation. Indicated for HR+/HER2- advanced breast cancer (with exemestane), advanced renal cell carcinoma, pancreatic/gastrointestinal/lung neuroendocrine tumors (NET), subependymal giant cell astrocytoma (SEGA), and renal angiomyolipoma with tuberous sclerosis; lower doses (0.25/0.5mg) are used for kidney and liver transplant rejection prophylaxis.