Letermovir
drugOn this page
Also known as AIC 246AIC-246AIC246MK-8228PrevymisC0088677
Summary
Letermovir (CHEMBL1241951) is an approved small molecule (ATC J05AX18); indicated across 5 conditions including cytomegalovirus infection and viral infectious disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: J05AX18
- Indications: 5 conditions
- Clinical trials: 46
- Chemistry: 572.5 Da · C29H28F4N4O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1241951 |
| Name | Letermovir |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 45138674 |
| ATC | J05AX18 |
| Molecular formula | C29H28F4N4O4 |
| Molecular weight | 572.5 |
| InChIKey | FWYSMLBETOMXAG-QHCPKHFHSA-N |
SMILES: COC1=C(C=C(C=C1)C(F)(F)F)N2[C@H](C3=C(C(=CC=C3)F)N=C2N4CCN(CC4)C5=CC(=CC=C5)OC)CC(=O)O
IUPAC name: 2-[(4S)-8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-4H-quinazolin-4-yl]acetic acid
Also known as: AIC 246, AIC-246, AIC246, Letermovir, MK-8228, Prevymis, LETERMOVIR, C0088677, letermovir
Patent coverage: 472 distinct patent families (1,026 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 918 (89%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 10 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Cholecystokinin receptor type A, Sodium channel protein type 5 subunit alpha, Progesterone receptor, 5-hydroxytryptamine receptor 1A, 5-hydroxytryptamine receptor 2A, Alpha-1A adrenergic receptor, Adenosine receptor A3, 3’,5’-cyclic-AMP phosphodiesterase 4D, Bile salt export pump.
Bioactivity
ChEMBL activities: 5 potent at pChembl ≥ 5 of 10 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ADRA1A | 5.72 | AC50 | 1900 | nM | CHEMBL_ACT_25218461 |
| HTR2A | 5.62 | AC50 | 2400 | nM | CHEMBL_ACT_25225667 |
| HTR1A | 5.23 | AC50 | 5900 | nM | CHEMBL_ACT_25216393 |
| CCKAR | 5 | AC50 | 10000 | nM | CHEMBL_ACT_25178724 |
| HTR2B | 5 | AC50 | 10040 | nM | CHEMBL_ACT_25228038 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
5 indications (3 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| cytomegalovirus infection | 4 | MONDO:0005132 | EFO:0001062 |
| viral infectious disease | 4 | MONDO:0005108 | EFO:0000763 |
| graft versus host disease | 2 | MONDO:0013730 | MONDO:0013730 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 46.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 15 |
| PHASE3 | 11 |
| Not specified | 10 |
| PHASE4 | 6 |
| PHASE1 | 3 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT05626530 | PHASE4 | RECRUITING | Letermovir for Secondary Prophylaxis in Solid Organ Transplant Recipients |
| NCT07235683 | PHASE4 | RECRUITING | Combination Letermovir and Standard of Care Antiviral for Enhanced Antiviral Response in Cytomegalovirus Infection in Lung Transplant Recipients |
| NCT07266467 | PHASE4 | RECRUITING | Efficacy and Safety of Leymovir Versus Valganciclovir in Prevention of Cytomegalovirus Infection and Cytomegalovirus Disease in Chinese Kidney Transplant Recipients |
| NCT07571135 | PHASE4 | NOT_YET_RECRUITING | Letermovir vs Valganciclovir in CMV R+ Kidney Transplant |
| NCT04904614 | PHASE4 | COMPLETED | Letermovir Use in Heart Transplant Recipients |
| NCT05914675 | PHASE4 | UNKNOWN | Letermovir for Primary Prophylaxis of Cytomegalovirus Infection After R+HID-HSCT |
| NCT05446571 | PHASE3 | RECRUITING | Prenatal Treatment of Congenital Cytomegalovirus Infection With Letermovir Versus Valaciclovir |
| NCT05711667 | PHASE3 | RECRUITING | A Study of the Drug Letermovir as Prevention of Cytomegalovirus Infection After Stem Cell Transplant in Pediatric Patients |
| NCT06334497 | PHASE3 | RECRUITING | Letermovir-based Dual Therapy for Treatment of Cytomegalovirus Infections |
| NCT06407232 | PHASE3 | RECRUITING | Letermovir (Prevymis) for CMV in Kidney and Pancreas Transplant Recipients |
| NCT06449586 | PHASE3 | ACTIVE_NOT_RECRUITING | CMV-specific T Cell Immunity Test Indicated Prophylaxis of Letermovir After All-HSCT |
| NCT07079735 | PHASE2/PHASE3 | RECRUITING | Valganciclovir vs. Letermovir for CMV Prophylaxis in Heart Transplant |
| NCT02137772 | PHASE3 | COMPLETED | Letermovir (MK-8228) Versus Placebo in the Prevention of Clinically-Significant Cytomegalovirus (CMV) Infection in Adult, CMV-Seropositive Allogeneic Hematopoietic Stem Cell Transplant Recipients (MK-8228-001) |
| NCT03443869 | PHASE3 | COMPLETED | Letermovir Versus Valganciclovir to Prevent Human Cytomegalovirus Disease in Kidney Transplant Recipients (MK-8228-002) |
| NCT03930615 | PHASE3 | COMPLETED | Extension of Letermovir (LET) From Day 100 to Day 200 Post-transplant for the Prevention of Cytomegalovirus (CMV) Infection in Hematopoietic Stem Cell Transplant (HSCT) Participants (MK-8228-040) |
| NCT04129398 | PHASE3 | COMPLETED | MK-8228 (Letermovir) in the Prevention of Human Cytomegalovirus (CMV) Infection and Disease in Adult Japanese Kidney Transplant Recipients (MK-8228-042) |
| NCT05763823 | PHASE3 | COMPLETED | A Study of Letermovir (MK-8228) to Evaluate Efficacy and Safety for Prevention of Cytomegalovirus Infection in Chinese Hematopoietic Stem Cell Transplant Recipients (MK-8228-045) |
| NCT06341686 | PHASE3 | UNKNOWN | Evaluation of the Prophylactic Use of Letermovir in Kidney Transplant Recipients at Risk of Cytomegalovirus Infection |
| NCT04060277 | PHASE2 | ACTIVE_NOT_RECRUITING | Triplex Vaccine in Preventing CMV Infection in Patients Undergoing Hematopoietic Stem Cell Transplantation |
| NCT05432778 | PHASE2 | RECRUITING | Cytomegalovirus Prophylaxis With Letermovir in Heart Transplant Recipients |
| NCT06453460 | PHASE2 | RECRUITING | CMV-TCIP Directed Letermovir Prophylaxis After Allo-SCT |
| NCT06575374 | PHASE2 | RECRUITING | Single Arm Pilot Trial of Letermovir for CMV Prophy in CAR T Cell |
| NCT06626555 | PHASE2 | NOT_YET_RECRUITING | Clinical Trial to Evaluate the Effects of Letermovir Prophylaxis on T-cell Immune Activation in Participants With Treated HIV-1 Infection |
| NCT06920251 | PHASE2 | RECRUITING | Phase II Trials of Letermovir Prophylaxis in Patients With RRMM Undergoing Elranatamab Therapy |
| NCT01063829 | PHASE2 | COMPLETED | Safety and Efficacy Study of a New Antiviral Drug to Prevent Cytomegalovirus Reactivation in Bone Marrow Transplanted Patients |
| NCT03728426 | PHASE2 | COMPLETED | Letermovir Treatment for Refractory or Resistant Cytomegalovirus Infection |
| NCT03940586 | PHASE2 | COMPLETED | Letermovir Treatment in Pediatric Participants Following Allogeneic Haematopoietic Stem Cell Transplantation (HSCT) (MK-8228-030) |
| NCT04017962 | PHASE2 | COMPLETED | A Study of the Drug Letermovir (LTV) as Prevention for Recurrent of Cytomegalovirus (CMV) Infection |
| NCT04312841 | PHASE2 | COMPLETED | Letermovir for the Prevention of Cytomegalovirus Reactivation in Patients With Hematological Malignancies Treated With Alemtuzumab |
| NCT04840199 | PHASE2 | TERMINATED | A Study to Evaluate the Anti-inflammatory Effects of Letermovir (Prevymis) in Adults With Human Immunodeficiency Virus (HIV)-1 and Asymptomatic Cytomegalovirus (CMV) Who Are on Suppressive Antiretroviral Therapy, Plus Its Effect on Chronic Inflammation, HIV Persistence and Other Clinical Outcomes. |
| NCT05041426 | PHASE2 | COMPLETED | Letermovir for CMV Prevention After Lung Transplantation |
| NCT05969743 | PHASE2 | UNKNOWN | Letermovir Prophylaxis for Cytomegalovirus (CMV) in Patients With Graft-versus-host Disease |
| NCT06021210 | PHASE2 | UNKNOWN | Letermovir for the Prevention of CMV Infection in HSCT Recipients Based on the Outcome of mNGS |
| NCT06118515 | PHASE1 | RECRUITING | A Safety Assessment of Oral Letermovir in Infants With Symptomatic Congenital Cytomegalovirus |
| NCT07020533 | PHASE1 | RECRUITING | A Vaccine (CMV-MVA Triplex Vaccine) for the Enhancement of CMV-Specific Immunity and the Prevention of CMV Viremia in Patients Undergoing Haploidentical Hematopoietic Stem Cell Transplant |
| NCT07199465 | PHASE1 | RECRUITING | A Clinical Study of Letermovir (MK-8228) in Children and Adolescents Who Receive a Kidney Transplant (KT) (MK-8228-077) |
| NCT06441669 | Not specified | RECRUITING | Effect of Letermovir Prophylaxis on CMV-specific Immune Reconstitution Post UCBT |
| NCT06639854 | Not specified | RECRUITING | The Use of Cytomegalovirus Cell Mediated Immunity to Optimize the Duration of Letermovir Prophylaxis in Hematopoietic Cell Transplant Recipients |
| NCT06812598 | Not specified | RECRUITING | Efficacy of Extended Letermovir Prophylaxis to Prevent CMV Reactivation in High-Risk Chinese Adults Undergoing Allogeneic HSCT |
| NCT07286461 | Not specified | NOT_YET_RECRUITING | VIROMARKERS GA n.101194735 - CMV and TTV Biomarkers Study Protocol |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 3 clinical and 6 variant annotation(s) for this drug (gene-keyed; see PharmGKB).
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).