CYCLOSPORINE
- CAS No.
- 79217-60-0
- Chemical Name:
- CYCLOSPORINE
- Synonyms
- CNP (1-22);CYCLOSPORIN;CYCLOSPRINE;Cyclosporins;Cyclosporine;Cyclosporine (Neoral);CYCLOSPORINE USP/EP/BP;79217-60-0 CYCLOSPORINE;Cyclosporine (NSC-290193);CYCLOSPORINE / CICLOSPORIN
- CBNumber:
- CB1150021
- Molecular Formula:
- C62H111N11O12
- Molecular Weight:
- 1202.61
- MOL File:
- 79217-60-0.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/7/2 8:55:00
| form | Solid |
|---|---|
| color | White to light yellow |
| BCS Class | 2,3,4 |
| CAS DataBase Reference | 79217-60-0(CAS DataBase Reference) |
| IARC | 1 (Vol. 50, 100A) 2012 |
CYCLOSPORINE Chemical Properties,Uses,Production
Description
Cyclosporine is a cyclic polypeptide with potent, partially selective immunosupressive activity. Isolated from the species Cylindrocarpon lucidium and Trichoderma polysporum, cyclosporine is useful in the prevention and treatment of graft/host disease and the prevention of rejection following organ transplantation. It appears to act by preferentially suppressing T-lymphocytes. Cyclosporine lacks myelotoxicity, although impaired renal and liver function have been observed. Initial administration is via the intravenous route, followed by oral maintenance therapy.
Chemical Properties
White crystalline solid or powder.
Indications
Cyclosporine (Sandimmune) is a potent inhibitor of antibody-
and cell-mediated immune responses and is the
immunosuppressant of choice for the prevention of
transplant rejection. It also has application in the treatment
of autoimmune diseases.
Cyclosporine is a highly stable 11-amino acid cyclic
polypeptide. The molecule is very lipophilic and essentially
is not soluble in water. It can be administered intravenously,
orally, or by injection.
Mechanism of action
Cyclosporine can bind to the cytosolic protein cytophilin
C. This drug–protein complex inhibits calcineurin
phosphatase activity, which leads to a decreased
synthesis and release of several cytokines,
including interleukins IL-2, IL-3, IL-4, interferon-, and
tumor necrosis factor.
Cyclosporine exhibits a high degree of specificity in
its actions on T cells without significantly impairing Bcell
activity. It can inhibit the T cell–dependent limb of
antibody production by lymphocytes by preventing the
differentiation of B cells into antibody-secreting plasma
cells. Because T cells appear to require IL-2 stimulation
for their continuous growth, cyclosporine impairs the
proliferative response of T cells to antigens. However,
once T cells have been stimulated by antigens to synthesize
IL-2, cyclosporine cannot suppress the proliferation
of T cells induced by this cytokine.
Pharmacology
After oral administration, cyclosporine is absorbed slowly and incompletely, with great variation among individuals. Peak plasma concentrations are reached in 3 to 4 hours, and the plasma half-life is 10 to 27 hours. The drug is extensively metabolized by hepatic mixedfunction oxidase enzymes and is excreted principally via the bile into the feces. Metabolism results in inactivation of the immunosuppressive activity.Agents that enhance or inhibit the mixed-function oxidase enzymes will alter the therapeutic response to cyclosporine.
Clinical Use
Cyclosporine has been approved for use in allogeneic
kidney, liver, and heart transplant patients and is under
study for use in pancreas, bone marrow, single lung, and
heart–lung transplant procedures. It is recommended
that corticosteroids, such as prednisone, be used concomitantly,
although at half or less of their usual dose.
Such combined therapy leads to fewer side effects, a decreased
incidence of infectious complications, efficacy
of lower doses of cyclosporine, and a better history of
patient survival.
Cyclosporine appears to have promise in the treatment
of autoimmune diseases. It has a beneficial effect
on the course of rheumatoid arthritis, uveitis, insulindependent
diabetes, systemic lupus erythematosus, and
psoriatic arthropathies in some patients. Toxicity is
more of a problem in these conditions than during use
in transplantation, since higher doses of cyclosporine
are often required to suppress autoimmune disorders.
Side effects
Compared with previously available therapy, the adverse effects associated with cyclosporine are much less severe but still worthy of concern. Nephrotoxicity, which can occur in up to 75% of patients, ranges from severe tubular necrosis to chronic interstitial nephropathy.This effect is generally reversible with dosage reduction. Vasoconstriction appears to be an important aspect of cyclosporine- induced nephrotoxicity. Hypertension occurs in 25% of the patients and more frequently in patients with some degree of renal dysfunction; the concomitant use of antihypertensive drugs may prove useful. Hyperglycemia, hyperlipidemia, transient liver dysfunction, and unwanted hair growth are also observed.
Potential Exposure
Cyclosporin A is a fungal metabolite; an amide immunosuppressant drug used in various surgeries.
Shipping
UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials.
Incompatibilities
Amides/imides react with azo and diazo compounds to generate toxic gases. Flammable gases are formed by the reaction of organic amides/imides with strong reducing agents such as hydrideds and active metals. Amides are very weak bases (weaker than water). Imides are less basic yet and in fact react with strong bases to form salts. That is, they can react as acids. Mixing amides with dehydrating agents such as such as phosphorus pent- oxide or thionyl chloride generates the corresponding nitrile. The combustion of these compounds generates mixed oxides of nitrogen (NOx).
Waste Disposal
t is inappropriate and possibly dangerous to the environment to dispose of expired or waste drugs and pharmaceuticals by flushing them down the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed with wet cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consider- ation applicable DEA, EPA, and FDA regulations. If possi- ble return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged, and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
CYCLOSPORINE Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Concord Biotech Limited | +91-2714398200 +91-2714398200 | Gujarat, India | 22 | 58 | Inquiry |
| Bills Biotech Pvt Ltd | +91-8980792545 +91-8238037545 | Gujarat, India | 4 | 58 | Inquiry |
| CONCORD BIOTECH LTD | +91 79 68138700 | New Delhi, India | 18 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Hebei Duling International Trade Co. LTD | +8617333973358 | China | 15438 | 58 | Inquiry |
| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 | China | 21676 | 55 | Inquiry |
| career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29901 | 58 | Inquiry |
| Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
| Shaanxi Dideu Medichem Co. Ltd | +86-029-81138252 +86-18789408387 | China | 2316 | 58 | Inquiry |
| JIAXING REGEN CHEMICAL CO.,LTD | +8613385739570 | China | 226 | 58 | Inquiry |
79217-60-0(CYCLOSPORINE)Related Search:
1of3
chevron_right