Drug target · HTR2A
5-HT2A
5-hydroxytryptamine receptor 2A
25 compounds in the CNS pipeline act on 5-HT2A.
Compounds targeting 5-HT2A
| Compound | Action | Affinity | Lead program | Developer |
|---|---|---|---|---|
| Lumateperone (ITI-007)primarySmall molecule | Antagonist | Ki 0.5 nM | ApprovedSchizophrenia | Intra-Cellular Therapies, Inc. |
| CYB003 (deupsilocin)primarySmall molecule | Agonist | — | Phase 3Major depressive disorder | Helus Pharma |
| Iloperidone LAIprimarySmall molecule | Antagonist | Ki 5.6 nM | Phase 3Schizophrenia | Vanda Pharmaceuticals Inc. |
| Lysergide D-tartrate (MM120 / LSD)primaryPsychedelic | Partial agonist | pKi 9.4 | Phase 3Generalized anxiety disorder | Definium Therapeutics, Inc. |
| Milsaperidone (VHX-896)primarySmall molecule | Antagonist | Ki 0.28 nM | Phase 3Major depressive disorder | Vanda Pharmaceuticals Inc. |
| Psilocybin (COMP360)primaryPsychedelic | Partial agonist | pEC50 7.6 | Phase 3Treatment-resistant depression | COMPASS Pathways plc |
| RemlifanserinprimarySmall molecule | Inverse agonist | — | Phase 3Alzheimer's disease psychosis | ACADIA Pharmaceuticals Inc. |
| Roluperidone (MIN-101)primarySmall molecule | Antagonist | Ki 8.19 nM | Phase 3Schizophrenia | Minerva Neurosciences, Inc. |
| Bretisilocin (GM-2505)primaryPsychedelic | Agonist | EC50 15 nM | Phase 2Major depressive disorder | Gilgamesh Pharmaceuticals, Inc. |
| CYB004 (deuterated DMT)primaryPsychedelic | Agonist | — | Phase 2Generalized anxiety disorder | Helus Pharma |
| ITI-1284 (deulumateperone)primarySmall molecule | Antagonist | — | Phase 2Agitation in Alzheimer's disease | Intra-Cellular Therapies, Inc. |
| Luvesilocin (RE104)primaryPsychedelic | Agonist | Ki 120 nM | Phase 2Postpartum depression | Reunion Neuroscience Inc. |
| Mebufotenin (inhaled 5-MeO-DMT, GH001)primaryPsychedelic | Agonist | — | Phase 2Treatment-resistant depression | GH Research PLC |
| MSP-1014primaryPsychedelic | Agonist | — | Phase 2Major depressive disorder | Mindset Pharma Inc. |
| VLS-01primaryPsychedelic | Agonist | — | Phase 2Treatment-resistant depression | Atai Beckley N.V. (AtaiBeckley) |
| ELE-101 (intravenous psilocin benzoate)primaryPsychedelic | Agonist | pEC50 7.6 | Phase 1/2Major depressive disorder | Beckley Psytech Limited |
| Zalsupindole (DLX-001)primarySmall molecule | Partial agonist | — | Phase 1Major depressive disorder | Delix Therapeutics, Inc. |
| TNX-102 SL (cyclobenzaprine HCl sublingual)Small molecule | Antagonist | Ki 5.2 nM | ApprovedFibromyalgia | Tonix Pharmaceuticals Holding Corp. |
| BrexpiprazoleSmall molecule | Antagonist | Ki 0.47 nM | Filed (NDA)Post-traumatic stress disorder | Otsuka Pharmaceutical Co., Ltd. |
| Olanzapine extended-release injectable suspension (TEV-'749)Small molecule | Antagonist | — | Filed (NDA)Schizophrenia | Teva Pharmaceutical Industries Ltd. |
| Brilaroxazine (RP5063)Small molecule | Partial agonist | Ki 2.5 nM | Phase 3Schizophrenia | Reviva Pharmaceuticals Holdings, Inc. |
| LYBALVI (olanzapine/samidorphan)Small molecule | Antagonist | Ki 4 nM | Phase 3Schizophrenia | Alkermes plc |
| NRX-101 (D-cycloserine/lurasidone)Small molecule | Antagonist | — | Phase 3Bipolar depression | NRx Pharmaceuticals, Inc. |
| BPL-003 (intranasal 5-MeO-DMT benzoate)Psychedelic | Agonist | — | Phase 2Treatment-resistant depression | Beckley Psytech Limited |
| DT402Psychedelic | Partial agonist | EC50 3100 nM | Phase 2Autism spectrum disorder | Definium Therapeutics, Inc. |