9-(N-methyl-L-isoleucine)-cyclosporin A
Also known as: [N-Me-Ile9]cyclosporin A, 9-MeIle-CsA, CsA‑9‑NMeIle, cyclosporin A, 9-(N-methyl-L-isoleucine)-, MeIle4-cyclosporin, N-methyl-4-isoleucine cyclosporin, NIM811, SDZ NIM 811
Source 9-(N-methyl-L-isoleucine)-cyclosporin A at Peptiology
Save 10% with code PEPTI-BOSSRABBIT-10
Tapping Shop Now & Save 10% copies your 10% off code PEPTI-BOSSRABBIT-10 to your clipboard. Paste it at the Peptiology checkout to claim the discount.
Summary
9-(N-methyl-L-isoleucine)-cyclosporin A is a synthetic analog of cyclosporin A in which the 9th residue is replaced by N‑methyl‑L‑isoleucine. It retains the cyclic 11‑residue backbone and is investigated for altered potency and pharmacokinetics.
Mechanism of Action
binds cyclophilin A, forming a complex that inhibits calcineurin, thereby suppressing T‑cell activation
Routes of Administration
Goals & Uses
- HIV-1 replication inhibitionAntiviralLow
- Cytoprotection via mPTP inhibitionCardioprotection / HepatoprotectionLow
- transplant rejection prophylaxisTherapeuticUnknown
- ImmunosuppressionTherapeuticModerate
- autoimmune disease treatmentTherapeuticUnknown
- Hepatitis C virus (HCV) suppressionAntiviralModerate
Contraindications
- Hypersensitivity to cyclosporin or cyclosporin analoguesAllergyHigh
- Severe hepatic impairmentOrganModerateLiver function concerns
Adverse Effects
- HepatotoxicityHepaticUnknownLiver injury or dysfunction
- NeurotoxicityNeurologicalUnknown
- HypertensionCardiovascularUnknownHigh blood pressure
- HeadacheNeurologicUncommonPain in the head or upper neck
- malignancy riskOncologicalUnknown
- Gastrointestinal disturbanceGastrointestinalCommon
- Elevated liver enzymesHepaticUncommonIncrease in AST/ALT or other hepatic markers
- NephrotoxicityRenalUnknown
- Infection susceptibilityImmunologicUnknown
Drug Interactions
- nephrotoxic drugsHigh
- CYP3A4 inhibitors/inducersModerate
- P-glycoprotein substrates/inhibitorsLow
- CYP3A4 inducers (e.g., rifampicin, carbamazepine)Moderate
- P-glycoprotein substratesModerate
- CYP3A4 inhibitors (e.g., ketoconazole, ritonavir)Moderate
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairmentOrgan ImpairmentRelative
- Severe renal impairmentOrgan ImpairmentRelative
- Pediatric populationAgeRelative
- Severe hepatic impairmentOrgan ImpairmentRelative
Regulatory Status
- European UnionUnapprovedNot in EMA database as approved product
- United StatesInvestigationalOnly used in preclinical and early‑phase clinical studies.
- United KingdomUnknownNo MHRA approval identified
Not listed in FDA Orange Book, EMA database, or major pharmacopeias as of knowledge cutoff. Appears in patent literature (e.g., Novartis cyclosporin analog patents) and research contexts but lacks established clinical development status.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is 9-(N-methyl-L-isoleucine)-cyclosporin A?
9-(N-methyl-L-isoleucine)-cyclosporin A is a synthetic analog of cyclosporin A in which the 9th residue is replaced by N‑methyl‑L‑isoleucine. It retains the cyclic 11‑residue backbone and is investigated for altered potency and pharmacokinetics.
What is 9-(N-methyl-L-isoleucine)-cyclosporin A used for?
9-(N-methyl-L-isoleucine)-cyclosporin A is educationally associated with: HIV-1 replication inhibition, Cytoprotection via mPTP inhibition, transplant rejection prophylaxis, Immunosuppression, autoimmune disease treatment, Hepatitis C virus (HCV) suppression. Educational only — not medical advice.
How is 9-(N-methyl-L-isoleucine)-cyclosporin A administered?
Recorded routes of administration: Intravenous, Oral.
What are the potential side effects of 9-(N-methyl-L-isoleucine)-cyclosporin A?
Reported adverse effects include: Hepatotoxicity, Neurotoxicity, Hypertension, Headache, malignancy risk, Gastrointestinal disturbance, Elevated liver enzymes, Nephrotoxicity, Infection susceptibility. This list is not exhaustive — consult a qualified clinician.
Who should avoid 9-(N-methyl-L-isoleucine)-cyclosporin A?
Recorded contraindications: Hypersensitivity to cyclosporin or cyclosporin analogues, Severe hepatic impairment. Consult a qualified clinician before use.