PPIDT00074

Drug Information
NameCyclosporine
SequenceNot Available
DrugBank_IDDB00091
Typesmall molecule
IndicationCyclosporine is approved for a variety of conditions. Firstly, it is approved for the prophylaxis of organ rejection in allogeneic kidney, liver, and heart transplants. It is also used to prevent bone marrow transplant rejection. For the above indications, cyclosporine can be used in conjunction with azathioprine and corticosteroids. Finally, cyclosporine can be used in patients who have chronic transplant rejection and have received previous immunosuppressive therapy[L3002] and to prevent or treat graft-versus-host disease (GVHD).[L11097] Secondly, cyclosporine is used for the treatment of patients with severe active rheumatoid arthritis (RA) when they no longer respond to methotrexate alone.[L3734] It can be used for the treatment of adult non-immunocompromised patients with severe, recalcitrant, plaque psoriasis that have failed to respond to at least one systemic therapy or when systemic therapies are not tolerated or contraindicated.[L3734] The ophthalmic solution of cyclosporine is indicated to increase tear production in patients suffering from keratoconjunctivitis sicca.[L11097] In addition, cyclosporine is approved for the treatment of steroid dependent and steroid-resistant nephrotic syndrome due to glomerular diseases which may include minimal change nephropathy, focal and segmental glomerulosclerosis or membranous glomerulonephritis.[L11097] A cyclosporine ophthalmic emulsion is indicated in the treatment of vernal keratoconjunctivitis in adults and children.[L34694] Off-label, cyclosporine is commonly used for the treatment of various autoimmune and inflammatory conditions such as atopic dermatitis, blistering disorders, ulcerative colitis, juvenile rheumatoid arthritis, uveitis, connective tissue diseases, as well as idiopathic thrombocytopenic purpura.[A139,A174085,A189393,A189396,A189399]
Dosage Forms
Form Route Strength
Solution Oral
1000000 g
Solution Ophthalmic
0.09 % w/v
Solution / drops Ophthalmic; Topical
0.0009 mg/1mL
Solution / drops Ophthalmic; Topical
0.0009 g/1mL
Solution / drops Ophthalmic
0.9 mg/ml
Solution / drops Ophthalmic
0.0005
Solution Oral
100 MG/ML
Solution Oral
10000000 mg
Solution / drops Ophthalmic
0.5 mg/ml
Liquid Topical
0.25 g/100mL
Capsule Oral
100 mg/1
Capsule, gelatin coated Oral
100 mg/1
Capsule, gelatin coated Oral
25 mg/1
Capsule, liquid filled Oral
100 mg/1
Injection, solution Intravenous
50 mg/1mL
Solution Oral
100 mg/1mL
Powder Not applicable
1 g/1g
Capsule, liquid filled Oral
25 mg/1
Capsule, liquid filled Oral
50 mg/1
Emulsion Ophthalmic
1 mg/1mL
Emulsion Ophthalmic
0.50 mg
Emulsion Ophthalmic
0.0005
Solution / drops Ophthalmic
0.001
Capsule, liquid filled Oral
100.00 MG
Capsule, liquid filled Oral
25.00 MG
Capsule, liquid filled Oral
50.00 MG
Capsule Oral
100.00 mg
Emulsion Oral
10.000 g
Emulsion Oral
10.00 g
Capsule Oral
50 mg
Capsule, liquid filled Oral
100 MG
Capsule, liquid filled Oral
25 MG
Capsule Oral
25 mg/1
Capsule Oral
50 mg/1
Liquid Ophthalmic
0.0005 g/100mL
— Ophthalmic
1 mg/ml
Liquid Ophthalmic
1 mg/1ml
Solution / drops Ophthalmic
1 MG/ML
Solution / drops Ophthalmic
Emulsion Ophthalmic
1 mg/ml
Capsule Oral
25.000 mg
Tablet Oral
2500000 mg
Solution Intravenous
50.000 mg
Solution Conjunctival; Ophthalmic
100000 mg
Solution Ophthalmic
1.000 mg
Solution Oral
Capsule Oral
Capsule Oral
25.00 mg
Emulsion Oral
100 mg
Capsule Oral
10 mg
Solution Oral
100 mg / mL
Capsule, gelatin coated Oral
100 mg
Capsule, gelatin coated Oral
25 mg
Capsule, gelatin coated Oral
50 mg
Emulsion Ophthalmic
0.05 % w/v
Emulsion Ophthalmic
0.5 mg/1mL
Emulsion Ophthalmic
0.500 mg
Emulsion Ophthalmic
0.05 % w/w
Emulsion Conjunctival
0.2 mg
Injection, solution, concentrate Intravenous; Parenteral
50 MG/ML
Solution Parenteral
0.05 g
Solution —
50 mg/1ml
Injection, solution, concentrate Parenteral
50 mg/ml
Injection, solution Intravenous
50 mg/ml
Injection Intravenous
50.0 mg/ml
Capsule Oral
50.000 mg
Capsule Oral
100 mg
Capsule Oral
25 mg
Capsule, liquid filled Oral
1000000 mg
Capsule, liquid filled Oral
10.0 mg
Capsule, liquid filled Oral
100.0 mg
Capsule, liquid filled Oral
25.0 mg
Capsule, liquid filled Oral
50.0 mg
Solution Oral
100.0 mg/ml
Emulsion Oral
10 g
Emulsion Oral
1000000 g
Capsule, liquid filled Oral
5000000 mg
Capsule, liquid filled Oral
2500000 mg
— Oral
100 mg/ml
Solution Intravenous
0.05 g
Capsule, liquid filled Oral
10000000 mg
Injection Intravenous
50 mg/1mL
Solution Intravenous
50 mg / mL
Liquid Oral
100 mg / mL
— Oral
Emulsion Ophthalmic
0.1 % w/v
Emulsion Ophthalmic; Topical
1 mg/1mL
Solution / drops Ophthalmic
1 mg/1mL
Solution —
10.00 mg
Target Information
Role Uniprot_ID Gene_Name Entity_Name Organism Actions Internal link
target P49069 CAMLG Guided entry of tail-anchored proteins factor CAMLG Homo sapiens binder Link
target Q08209 PPP3CA Protein phosphatase 3 catalytic subunit alpha Homo sapiens inhibitor Link
target Q96LZ3 PPP3R2 Calcineurin subunit B type 2 Homo sapiens inhibitor Link
target P62937 PPIA Peptidyl-prolyl cis-trans isomerase A Homo sapiens inhibitor|binder Link
target P30405 PPIF Peptidyl-prolyl cis-trans isomerase F, mitochondrial Homo sapiens binder Link
enzyme P33261 CYP2C19 Cytochrome P450 2C19 Homo sapiens inhibitor Link
enzyme P10635 CYP2D6 Cytochrome P450 2D6 Homo sapiens inhibitor Link
enzyme P20815 CYP3A5 Cytochrome P450 3A5 Homo sapiens substrate Link
enzyme P08684 CYP3A4 Cytochrome P450 3A4 Homo sapiens substrate|inhibitor Link
transporter P08183 ABCB1 ATP-dependent translocase ABCB1 Homo sapiens substrate|inhibitor Link
transporter O95342 ABCB11 Bile salt export pump Homo sapiens substrate|inhibitor Link
transporter Q12908 SLC10A2 Ileal sodium/bile acid cotransporter Homo sapiens inhibitor Link
transporter Q14973 SLC10A1 Hepatic sodium/bile acid cotransporter Homo sapiens inhibitor Link
transporter Q4U2R8 SLC22A6 Solute carrier family 22 member 6 Homo sapiens substrate|inhibitor Link
transporter Q5T3U5 ABCC10 ATP-binding cassette sub-family C member 10 Homo sapiens substrate|inhibitor Link
transporter Q92887 ABCC2 ATP-binding cassette sub-family C member 2 Homo sapiens inhibitor Link
transporter Q9UNQ0 ABCG2 Broad substrate specificity ATP-binding cassette transporter ABCG2 Homo sapiens inhibitor Link
transporter Q9Y6L6 SLCO1B1 Solute carrier organic anion transporter family member 1B1 Homo sapiens substrate|inhibitor Link
transporter Q9NPD5 SLCO1B3 Solute carrier organic anion transporter family member 1B3 Homo sapiens inhibitor Link