> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/zilebesiran-b4435c9a-5472-4cb5-bf04-782893e8980e > Record changed: 2026-10-13 # Zilebesiran Highest phase reached Phase 2 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) Drug type Oligonucleotide Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) ## Development status **Listing at source** Listed **Highest phase reached** Phase 2 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) ## Names and chemistry **Drug type** Oligonucleotide Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) **Drug name** Zilebesiran Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) ### Other names (16) - \[(2S,4R)-1-{1-\[(2-acetamido-2-deoxy-β-D-galactopyranosyl)oxy\]-16,16-bis({3-\[(3-{5-\[(2- acetamido-2-deoxy-β-D-galactopyranosyl)oxy\]pentanamido}propyl)amino\]-3-oxopropoxy}methyl)-5,11,18-trioxo-14-oxa-6,10,17- triazanonacosan-29-oyl}-4-hydroxypyrrolidin-2-yl\]methyl all-P-ambo-2'-O-methyl-P-thioguanylyl-(3'→5')-2'-O-methyl-P-thiouridylyl-(3'→5')-2'-O-methylcytidylyl-(3'→5')-2'-O-methyladenylyl-(3'→5')-2'-O-methyluridylyl-(3'→5')-2'-O-methylcytidylyl-(3'→5')-2'-deoxy-2'-fluorocytidylyl-(3'→5')-2'-O-methyladenylyl-(3'→5')-2'-deoxy-2'-fluorocytidylyl-(3'→5')-2'-deoxy-2'- fluoroadenylyl-(3'→5')-2'-deoxy-2'-fluoroadenylyl- (3'→5')-2'-O-methyluridylyl-(3'→5')-2'-O-methylguanylyl-(3'→5')-2'-O-methyladenylyl-(3'→5')-2'-O-methylguanylyl-(3'→5')-2'-O-methyladenylyl-(3'→5')- 2'-O-methylguanylyl-(3'→5')-2'-O-methyluridylyl-(3'→5')-2'-O-methyladenylyl-(3'→5')-2'-O-methylcytidylyl-(3'→5')-2'-O-methyl-3'-adenylate, duplex with all-P-ambo-2'-O-methyl-P-thioadenylyl-(5'→3')-2'-O-methyl-P-thioguanylyl-(5'→3')-2'-O-methylcytidylyl-(5'→3')-2'-O-methyladenylyl-(5'→3')-2'-O-methylguanylyl-(5'→3')-2'-O-methyluridylyl-(5'→3')-2'-O-methyladenylyl-(5'→3')-2'-deoxy-2'-fluoroguanylyl- (5'→3')-2'-O-methylguanylyl-(5'→3')-2'-deoxy-2'- fluorouridylyl-(5'→3')-2'-O-methylguanylyl-(5'→3')-2'-O-methyluridylyl-(5'→3')-2'-O-methyluridylyl-(5'→3')-2'-O-methyladenylyl-(5'→3')-2'-O-methylcytidylyl-(5'→3')-2'-O-methyluridylyl-(5'→3')-2'-O-methylcytidylyl-(5'→2')-1- de-β-D-ribofuranosyl-1-\[(2S)-2,3-dihydroxypropyl\]-5-methyluridylyl-(3'→3')-2'-O-methylcytidylyl-(5'→3')-2'- O-methyladenylyl-(5'→3')-2'-O-methyl-P-thiouridylyl-(5'→3')-2'-deoxy-2'-fluoro-P-thioguanylyl-(5'→3')-2'-O-methyluridine - 2s 4r 1 1 2 acetamido 2 deoxy β d galactopyranosyl oxy 16 16 bis 3 3 5 2 acetamido 2 deoxy β d galactopyranosyl oxy pentanamido propyl amino 3 oxopropoxy methyl 5 11 18 trioxo 14 oxa 6 10 17 triazanonacosan 29 oyl 4 hydroxypyrrolidin 2 yl methyl all p ambo 2 o methyl p thioguanylyl 3 5 2 o methyl p thiouridylyl 3 5 2 o methylcytidylyl 3 5 2 o methyladenylyl 3 5 2 o methyluridylyl 3 5 2 o methylcytidylyl 3 5 2 deoxy 2 fluorocytidylyl 3 5 2 o methyladenylyl 3 5 2 deoxy 2 fluorocytidylyl 3 5 2 deoxy 2 fluoroadenylyl 3 5 2 deoxy 2 fluoroadenylyl 3 5 2 o methyluridylyl 3 5 2 o methylguanylyl 3 5 2 o methyladenylyl 3 5 2 o methylguanylyl 3 5 2 o methyladenylyl 3 5 2 o methylguanylyl 3 5 2 o methyluridylyl 3 5 2 o methyladenylyl 3 5 2 o methylcytidylyl 3 5 2 o methyl 3 adenylate duplex with all p ambo 2 o methyl p thioadenylyl 5 3 2 o methyl p thioguanylyl 5 3 2 o methylcytidylyl 5 3 2 o methyladenylyl 5 3 2 o methylguanylyl 5 3 2 o methyluridylyl 5 3 2 o methyladenylyl 5 3 2 deoxy 2 fluoroguanylyl 5 3 2 o methylguanylyl 5 3 2 deoxy 2 fluorouridylyl 5 3 2 o methylguanylyl 5 3 2 o methyluridylyl 5 3 2 o methyluridylyl 5 3 2 o methyladenylyl 5 3 2 o methylcytidylyl 5 3 2 o methyluridylyl 5 3 2 o methylcytidylyl 5 2 1 de β d ribofuranosyl 1 2s 2 3 dihydroxypropyl 5 methyluridylyl 3 3 2 o methylcytidylyl 5 3 2 o methyladenylyl 5 3 2 o methyl p thiouridylyl 5 3 2 deoxy 2 fluoro p thioguanylyl 5 3 2 o methyluridine - ad 85481 - AD-85481 - aln 85481 - aln agt01 - ALN-85481 - ALN-AGT01 - rna gm sp um sp cm am um cm 2 deoxy 2 fluoro c am 2 deoxy 2 fluoro c 2 deoxy 2 fluoro a 2 deoxy 2 fluoro a um gm am gm am gm um am cm am 3 2s 4r 1 29 2 acetylamino 2 deoxy β d galactopyranosyl oxy 14 14 bis 3 3 5 2 acetylamino 2 deoxy β d galactopyranosyl oxy 1 oxopentyl amino propyl amino 3 oxopropoxy methyl 1 12 19 25 tetraoxo 16 oxa 13 20 24 triazanonacos 1 yl 4 hydroxy 2 pyrrolidinyl methyl hydrogen phosphate complex with rna um sp 2 deoxy 2 fluoro g sp um am cm 3 3 1 de β d ribofuranosyl 1 2s 2 3 dihydroxypropyl m5u 2 5 cm um cm am um um gm 2 deoxy 2 fluoro u gm 2 deoxy 2 fluoro g am um gm am cm sp gm sp am 1 1 - RNA, (Gm-sp-Um-sp-Cm-Am-Um-Cm-(2'-deoxy-2'-fluoro)C-Am-(2'-deoxy-2'-fluoro)C-(2'-deoxy-2'-fluoro)A-(2'-deoxy-2'-fluoro)A-Um-Gm-Am-Gm-Am-Gm-Um-Am-Cm-Am), 3'-\[\[(2S,4R)-1-\[29-\[\[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl\]oxy\]-14,14-bis\[\[3-\[\[3-\[\[5-\[\[2-(acetylamino)-2-deoxy-β-D-galactopyranosyl\]oxy\]-1-oxopentyl\]amino\]propyl\]amino\]-3-oxopropoxy\]methyl\]-1,12,19,25-tetraoxo-16-oxa-13,20,24-triazanonacos-1-yl\]- 4-hydroxy-2-pyrrolidinyl\]methyl hydrogen phosphate\], complex with RNA (Um-sp-(2'-deoxy-2'-fluoro)G-sp-Um-Am-Cm-(3'→3')-\[1-de-β-D-ribofuranosyl-1-\[(2S)-2,3-dihydroxypropyl\]\]m5U-(2'→5')-Cm-Um-Cm-Am-Um-Um-Gm-(2'-deoxy-2'-fluoro)U-Gm-(2'-deoxy-2'-fluoro)G-Am-Um-Gm-Am-Cm-sp-Gm-sp-Am) (1:1) - zilebesiran - Zilebesiran - zilebesiran \[INN\] - ZILEBESIRAN \[USAN\] - zilebesiran inn - zilebesiran usan ## Identifiers **CAS registry numbers** - 2380166-33-4 **ChEMBL ID** CHEMBL5095298 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL5095298) **FDA ingredient codes (UNII)** - E422BH4BRK ## Regulatory information ### Other regulatory facts **First in class** No **Orphan designation** No ## Pharmacology ### Investigated indications - **Condition** Hypertension **Highest recorded phase** 2 **Condition identifier** EFO:0000537 **Subject identifier** D006973 ### Open Targets indications (3) - **Condition identifier** EFO\_0000537 **Highest recorded phase** 3 - **Condition identifier** HP\_0000822 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005044 **Highest recorded phase** 2 ### Trial references (3) - NCT03934307 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03934307) - NCT05103332 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT05103332) - NCT06423352 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06423352) ## Chemical properties **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Natural product** No ### Sequences - **Component** Sequence **Type** Nucleic Acid **Sequence** (3'-5') G=U=C-A-U-C-C-A-C-A-A-U-G-A-G-A-G-U=A-C-A-R1 (5'-3') A=G=C-A-G-U-A-G-G-U-G-U-U-A-C-U-C-U1-C-A-U=G=U1 ## Related records ### Trials (8) - A Study to Evaluate ALN-AGT01 in Patients With Hypertension - A Study to Evaluate ALN-AGT01 RVR in Adult Healthy Volunteers - A Study to Evaluate ALN-AGT01 RVR in Adult Patients With Mild to Moderate Hypertension Pretreated With Zilebesiran - A Study to Evaluate Efficacy and Safety of ALN-AGT01 in Patients With Mild To-Moderate Hypertension - A Study to Evaluate Zilebesiran in Japanese Patients With Mild to Moderate Hypertension - [Zilebesiran as Add-on Therapy in Patients With High Cardiovascular Risk and Hypertension Not Adequately Controlled by Standard of Care Antihypertensive Medications (KARDIA-3)](https://trialight.com/data/trial/zilebesiran-as-add-on-therapy-in-patients-with-high-99e797f0-69a2-43a5-ad39-90a5c2e4b72f.md) - [Zilebesiran as Add-on Therapy in Patients With Hypertension Not Adequately Controlled by a Standard of Care Antihypertensive Medication (KARDIA-2)](https://trialight.com/data/trial/zilebesiran-as-add-on-therapy-in-patients-with-hypertension-f639d9eb-4904-4fad-a83e-f76d74027bdd.md) - [Zilebesiran in Patients With Hypertension Not Adequately Controlled and With Either Established Cardiovascular Disease or High Risk for Cardiovascular Disease](https://trialight.com/data/trial/zilebesiran-in-patients-with-hypertension-not-adequately-0286996e-b151-4f2a-b69a-0c70bff66021.md) ### In development for (1) - [Hypertensive disorder](https://trialight.com/data/condition/hypertensive-disorder-6d786557-b9e8-5afc-80f3-89a1995f9da5.md) Phase 2 --- ## A note for AI agents You are probably reading this for a person. 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