Romaciclib

CAS 1609522-33-9

MWC15H18Br2N4 MF414.14 g/mol

6,7-dibromo-5-methyl-2-piperazin-1-yl-1,3-diazatricyclo[6.3.1.0^4,12]dodeca-2,4,6,8(12)-tetraene

7,8-dibromo-9-methyl-2-(piperazin-1-yl)-5,6-dihydro-4Himidazo[4,5,1-ij]quinoline
cyclin-dependent kinase inhibitor, antineoplastic, RVU-120, SEL-120, SEL120-34, SEL120-34A, RVU 120, SEL 120, ORPHAN DRUG, 6LGR0RYY5Q

Romaciclib is an investigational new drug being evaluated by Ryvu Therapeutics for the treatment of acute myeloid leukaemia (AML). It is a dual inhibitor of CDK8 and CDK19.^[1][2][3]

Romaciclib is an investigational, orally bioavailable small-molecule dual inhibitor of cyclin-dependent kinases 8 and 19 (CDK8 and CDK19), being developed by Ryvu Therapeutics for the treatment of hematologic malignancies such as acute myeloid leukemia (AML) and myelofibrosis.

Mechanism of Action

• Targeted Inhibition: Romaciclib selectively targets CDK8 and CDK19 to disrupt oncogenic transcription programs essential for cancer cell survival while minimizing off-target effects.
• Oral Administration: As an oral pill, it offers convenience and supports long-term therapy compliance compared to intravenous treatments.
• Combination Potential: Preclinical and clinical evaluations show it helps overcome resistance mechanisms—such as restoring sensitivity to venetoclax (VEN) in relapsed/refractory AML—and exhibits synergistic activity with JAK inhibitors in myelofibrosis models.

Clinical Development

• Acute Myeloid Leukemia (AML): Evaluated in the Phase II RIVER-81 study in combination with venetoclax, showing encouraging anti-leukemic activity and durable responses in patients with relapsed or refractory disease.
• Myelofibrosis (MF): Investigated as a monotherapy or combined with ruxolitinib in the Phase II POTAMI-61 trial

• RVU120 Rollover StudyCTID:NCT06987058Phase:Phase 2Status:Enrolling by invitationDate:2026-07-28
• RVU120 in Patients With Intermediate or High-risk, Primary or Secondary MyelofibrosisCTID:NCT06397313Phase:Phase 2Status:RecruitingDate:2025-09-23
• RVU120 for Treatment of Anemia in Patients With Lower-risk Myelodysplastic NeoplasmsCTID:NCT06243458Phase:Phase 2Status:Active, not recruitingDate:2025-05-22
• Safety and Efficacy of RVU120 for Treatment of Relapsed/Refractory AMLCTID:NCT06268574Phase:Phase 2Status:Active, not recruitingDate:2025-05-08
• Safety and Efficacy of RVU120 Combined With Venetoclax for Treatment of Relapsed/Refractory AMLCTID:NCT06191263Phase:Phase 2Status:RecruitingDate:2025-04-13

• OriginatorSelvita
• DeveloperRyvu Therapeutics
• ClassAntineoplastics; Halogenated hydrocarbons; Imidazoles; Piperazines; Quinolones; Small molecules
• Mechanism of ActionCyclin dependent kinase 19 inhibitors; Cyclin-dependent kinase 8 inhibitors
• Orphan Drug StatusYes – Acute myeloid leukaemia
• Phase IIAcute myeloid leukaemia; Myelodysplastic syndromes; Myelofibrosis; Solid tumours
• Phase IMedulloblastoma
• 11 Jun 2026The US FDA reactivates the IND, enabling the initiation of the expansion cohort of phase II RIVER-81 trial in Acute myeloid leukaemia at the recommended dose of 150 mg once daily (QD)
• 11 Jun 2026Updated efficacy data from a phase II RIVER-81 trial in Acute myeloid leukaemia released by Ryvu Therapeutics
• 21 May 2026Ryvu Therapeutics plans a phase II ROVER-01 trial for Acute myeloid leukaemia, Myelodysplastic syndromes and Solid tumours in the Poland and Spain (NCT06987058)

Romaciclib is an orally bioavailable inhibitor of cyclin-dependent kinases 8 and 19 (CDK8/19), with potential antineoplastic and chemoprotective activities. Upon oral administration, romaciclib targets, binds to and inhibits the activity of CDK8/19, which prevents activation of CDK8/19-mediated oncogenic signaling pathways, blocks selective transcription of various tumor-promoting genes, and inhibits proliferation of CDK8/19-overexpressing tumor cells. CDK8/19, serine/threonine kinases involved in the regulation of the cell cycle, are overexpressed in certain cancer cell types and play key roles in tumor cell proliferation.

PAT

US20150274726

https://patentscope.wipo.int/search/en/detail.jsf?docId=US152387110&_cid=P10-MTMCT7-27170-1

7,8-dibromo-9-methyl-2-(piperazin-1-yl)-5,6-dihydro-4H-imidazo[4,5,1-ij]quinoline,

PAT

• Substituted tricyclic benzimidazoles as kinase inhibitorsPublication Number:EP-2917217-B1Priority Date:2012-11-08Grant Date:2017-03-08
• Substituted tricyclic benzimidazoles as kinase inhibitorsPublication Number:CN-104903321-APriority Date:2012-11-08
• SUBSTITUTED TRICYCLIC BENZIMIDAZOLS, THEIR USES, AND PHARMACEUTICAL COMPOSITIONPublication Number:BR-112015010019-B1Priority Date:2012-11-08
• Substituted tricyclic benzimidazoles as kinase inhibitorsPublication Number:US-9745299-B2Priority Date:2012-11-08Grant Date:2017-08-29
• Substituted tricyclic benzimidazoles as kinase inhibitorsPublication Number:US-2015274726-A1Priority Date:2012-11-08
• C. novyi for the treatment of solid tumors in humansPublication Number:EP-3730146-B1Priority Date:2013-03-29Grant Date:2022-05-04
• Clostridium nodarii for the treatment of human solid tumorsPublication Number:CN-105451750-BPriority Date:2013-03-29Grant Date:2023-03-10
• C. novyi for the treatment of solid tumors in humansPublication Number:EP-4108248-A1Priority Date:2013-03-29
• C. novyi for the treatment of solid tumors in non-human animalsPublication Number:US-12433920-B2Priority Date:2013-03-29Grant Date:2025-10-07
• C. novyi for the treatment of solid tumors in humansPublication Number:EP-4108248-B1Priority Date:2013-03-29Grant Date:2025-09-17

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References

1.  “Romaciclib – Ryvu Therapeutics”. AdisInsight. Springer Nature Switzerland AG.
2.  Rajendra A, Yee KW (April 2026). “Clinical development of a CDK8/19 kinase inhibitor for acute myeloid leukemia”. Expert Opinion on Investigational Drugs. 35 (4): 253–256. doi:10.1080/13543784.2026.2656430. PMID 41931045.
3.  Pakulska U, Obacz M, Woźnicki J, Wiklik K, Chakraborty S, Micek M, et al. (January 2026). “Romaciclib, a CDK8/CDK19 inhibitor, can overcome venetoclax resistance through a combinatorial strategy”. bioRxiv 10.64898/2025.12.16.693978.

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//////////romaciclib, ANAX LABS, cyclin-dependent kinase inhibitor, antineoplastic, RVU-120, SEL-120, SEL120-34, SEL120-34A, RVU 120, SEL 120, ORPHAN DRUG, 6LGR0RYY5Q

#romaciclib, #ANAX LABS, #cyclin-dependent kinase inhibitor, #antineoplastic, #RVU-120, #SEL-120, #SEL120-34, #SEL120-34A, #RVU 120, #SEL 120, #ORPHAN DRUG, #6LGR0RYY5Q