Romaciclib

 

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.

• Cyclin-Dependent Kinase 8: A New Hope in Targeted Cancer Therapy?Publication Name:Journal of Medicinal ChemistryPublication Date:2017-12-21PMID:29266937DOI:10.1021/acs.jmedchem.7b00901
• SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domainsPublication Name:OncotargetPublication Date:2017-04-04PMCID:PMC5464911PMID:28422713DOI:10.18632/oncotarget.16810

• Discovery of a Novel and Potent Cyclin-Dependent Kinase 8/19 (CDK8/19) Inhibitor for the Treatment of CancerPublication Name:Journal of Medicinal ChemistryPublication Date:2024-05-01PMID:38690856DOI:10.1021/acs.jmedchem.4c00248
• Discovery of a novel oral type Ⅰ CDK8 inhibitor against acute myeloid leukemiaPublication Name:European Journal of Medicinal ChemistryPublication Date:2023-05-05PMID:36889252DOI:10.1016/j.ejmech.2023.115214
• Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Inhibitors of CDK8 for the Treatment of CancerPublication Name:Journal of Medicinal ChemistryPublication Date:2023-04-07PMID:37029334DOI:10.1021/acs.jmedchem.2c01718
• From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer TherapyPublication Name:Journal of Medicinal ChemistryPublication Date:2022-04-29PMID:35485642DOI:10.1021/acs.jmedchem.1c02064
• A comprehensive insight on the recent development of Cyclic Dependent Kinase inhibitors as anticancer agentsPublication Name:European Journal of Medicinal ChemistryPublication Date:2020-10-01PMID:32707525DOI:10.1016/j.ejmech.2020.112571

//////////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

Rocavorexant

 

Rocavorexant

CAS 2115665-09-1

MFC18H19F3N8O MW420.39

N,6-dimethyl-3-(2H-1,2,3-triazol-2-yl)-N-[(2S)-1-{[5-(trifluoromethyl)pyrazin-2-yl]amino}propan-2-yl]pyridine-2-
carboxamide
orexin-1 receptor antagonist, INDV-2000, C4X-3256, INDV 2000, C4X 3256,

Rocavorexant (developmental codes INDV-2000 and C4X-3256) is a potent, selective, oral orexin-1 receptor (OX₁R) antagonist originally developed to treat opioid use disorder and other substance-related disorders.

Clinical development of the drug has been suspended. In April 2026, Indivior announced that it would not advance the drug internally for opioid use disorder because the Phase 2 proof-of-concept trial failed to meet its primary endpoint of "no treatment failure".

Key Drug Profile

• Mechanism of Action: Highly selective antagonist for the human orexin-1 receptor (pIC50 of 9.1) compared to the orexin-2 receptor (pIC50 of 6.0).
• Target Pathway: Aims at relapse-related neural circuitry, anxiety modulation, and stress-induced addictive behaviors.
• Chemical Formula: C₁₈H₁₉F₃N₈O.
• Current Status: Suspended internally by Indivior, which is actively seeking external business development and out-licensing opportunities due to positive secondary data regarding abstinence and safet

Rocavorexant (INNTooltip International Nonproprietary Name; developmental code names C4X-3256 and INDV-2000) is an orexin OX₁ receptor antagonist which is under development for the treatment of opioid-related disorders and other substance-related disorders.^[1][2][3][4] It is taken orally.^[1] The drug is under development by C4X Discovery and/or Indivior.^[1][2] As of May 2026, development for all indications has been suspended.^[1] The drug has reached phase 2 clinical trials for opioid-related disorders and phase 1 trials for substance-related disorders.^[1][2][4]

Rocavorexant is the antagonist for orexin-1 receptor with pIC₅₀ of 9.1 for human OX1 (while pIC₅₀ for human OX2 is 6.0).

1. Primary patent — most important reference

WO2017129829A1 — “Therapeutic compounds”
Inventor: Barrie P. Martin
Priority: 29 January 2016
Publication: 3 August 2017

WO2017129829A1 – Google Patents

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2017129829&_cid=P12-MTJHA5-23107-1

This patent explicitly identifies Rocavorexant as:

N,6-dimethyl-3-(2H-1,2,3-triazol-2-yl)-N-[(2S)-1-{[5-(trifluoromethyl)pyrazin-2-yl]amino}propan-2-yl]pyridine-2-carboxamide, and provides its preparation as Example 1.

The patent is particularly useful because it contains large-scale examples, not merely milligram medicinal-chemistry experiments.

Preparation of A/,6-dimethyl-3-(2H-1 ,2,3-triazol-2-yl)-A/-r(2S)-1 -f r5-(trifluoro methyl)pyrazin-2-yllamino)propan-2-yllpyridine-2-carboxamide (Example 1 , Scheme 3)

---

To a stirred solution of Int 11 (0.58 g, 2.1 mmol) in THF (2 mL) was added DIPEA (1 .0 mL, 5.8 mmol) followed by 2-chloro-5-(trifluoromethyl)pyrazine (0.39 g, 2.1 mmol) and the mixture was heated at 70 °C for 4 hrs. The reaction mixture was allowed to cool to ambient temperature and allowed to stand over the weekend. The reaction mixture was heated at 70 °C for a further 4 hrs with stirring and allowed to cool to ambient temperature. The reaction mixture was evaporated in vacuo. The residue was purified by preparative HPLC (Column: Waters Xbridge C18 (10 μιτι, 30 x 100 mm). Conditions: Water + 0.2% ammonium hydroxide [Eluent A]; MeCN + 0.2% ammonium hydroxide [Eluent B]. Gradient: 10 to 95% B) and then lyophilised to give title compound as a white solid (0.32 g)

LCMS (Method C): Two peaks at 4.20 and 4.39 min, 421 [M+H]⁺

1 H NMR (500 MHz, d4-MeOH) δ 8.38 (d, 0.15 H), 8.34 (bs, 0.15 H), 8.24 (d, 0.85 H), 8.03 (bs, 0.85 H), 7.99 (s, 0.30 H), 7.97 (s, 1 .70 H), 7.85 (bs, 1 .00 H), 7.57 (d, 0.15 H),

7.41 (d, 0.85 H), 4.98 (m, 0.15 H), 4.06 (bm, 0.85 H), 3.50 (d, 0.15 H), 3.47 (d, 0.85 H),

3.42 (d, 0.85 H), 3.39 (d, 0.15 H), 3.05 (s, 2.55 H), 2.83 (s, 0.45 H), 2.65 (s, 0.45 H), 2.45 (bs, 2.55 H), 1 .38 (d, 0.45 H), 1 .07 (bs, 2.55 H). Preparation of A/,6-dimethyl-3-(2H-1 ,2,3-triazol-2-yl)-A/-r(2S)-1 -U5-(trifluoro methyl)pyrimidin-2-yllamino)propan-2-yllpyridine-2-carboxamide

---

---

US patent

US 11,130,746 B2 — Therapeutic compounds

US11130746B2 – Google Patents

This is especially relevant because its claims specifically cover processes for preparing the compounds, including:

Route A: reaction of the pyridine acid/lithium salt with an amide-coupling reagent and the chiral amine.

Route B: reaction of
N-[(2S)-1-aminopropan-2-yl]-N,6-dimethyl-3-(2H-1,2,3-triazol-2-yl)pyridine-2-carboxamide
with an appropriate heteroaryl leaving-group compound in the presence of a base.

The patent specifically lists thionyl chloride among the coupling reagents and DIPEA as an appropriate base for the heteroaryl substitution route.

---

Other patent-family references

• US 10,696,654 B2
• US 11,130,746 B2
• US 11,753,398
• US 12,441,709 B2

The later US family documents retain the Rocavorexant compound/process disclosure. For example, US10696654B2 reproduces the Example 1 synthesis and the Int 14 preparation.

---

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References

1.  "Rocavorexant". AdisInsight. 12 May 2026. Retrieved 5 June 2026.
2.  "Delving into the Latest Updates on Rocavorexant with Synapse". Synapse. 9 May 2026. Retrieved 5 June 2026.
3.  Raymond JS, Vareed RD, Peters J, James MH (October 2025). "Found in translation: orexin receptor antagonism for the treatment of opioid use disorder". Translational Psychiatry. 15 (1) 432. doi:10.1038/s41398-025-03571-5. PMC 12552597. PMID 41136352.
4.  Lorente JS, Sokolov AV, Ferguson G, Schiöth HB, Hauser AS, Gloriam DE (June 2025). "GPCR drug discovery: new agents, targets and indications". Nature Reviews. Drug Discovery. 24 (6): 458–479. doi:10.1038/s41573-025-01139-y. PMID 40033110.

Clinical data
Other names	C4X-3256; C4X3256; INDV-2000; INDV2000
Routes of administration	Oral[1]
Drug class	Orexin OX1 receptor antagonist
Identifiers
IUPAC name
CAS Number	2115665-09-1
PubChem CID	130295635
ChemSpider	133325612
UNII	8RJN30TJM6
KEGG	D13324
Chemical and physical data
Formula	C18H19F3N8O
Molar mass	420.400 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

////rocavorexant, anax labs, orexin-1 receptor antagonist, INDV-2000, C4X-3256, INDV 2000, C4X 3256,

#rocavorexant, #anax labs, #orexin-1 receptor antagonist, #INDV-2000, #C4X-3256, #INDV 2000, #C4X 3256,

Rizavasertib

 

Rizavasertib

CAS 552325-16-3

MF C24H23N5O MW397.5 g/mol

(2S)-1-(1H-indol-3-yl)-3-[[5-(3-methyl-2H-indazol-5-yl)-3-pyridinyl]oxy]propan-2-amine

(2S)-1-(1H-indol-3-yl)-3-{[5-(3-methyl-1H-indazol-5-yl)pyridin-3-yl]oxy}propan-2-amine
serine/threonine kinase inhibitor, A-443654, A 443654, A443654, Q4UG565ZYH

Rizavasertib was a drug candidate originally developed by Abbott (now AbbVie).^[1][2][3][4] It is a pan akt Inhibitor.^[5] It is now used as an akt inhibitor tool compound.^[6]

Rizavasertib (also known by its developmental code A-443654) is a potent, small-molecule pan-Akt (protein kinase B) inhibitor originally developed by Abbott Laboratories (now AbbVie). It acts as a highly effective research tool compound used to investigate cellular signaling pathways, particularly in oncology and tumor cell biology

• Mechanism of Action: It is an ATP-competitive inhibitor that targets all three Akt isoforms (Akt1, Akt2, and Akt3) with equal intracellular potency, showing an inhibition constant (\(\text{K}_{i}\)) of 160 pM.

Key Biological & Research Effects

• Pathway Modulation: It induces a rapid, paradoxical phosphorylation of Akt at the Ser-473 residue, occurring independently of mTORC1 inhibition.
• Mitotic Regulation: The compound interferes with normal cell division (mitotic progression) by regulating the expression of Aurora A kinase.
• Oncology Models: In preclinical testing, it has demonstrated an ability to prolong survival in animal models of intracranial glioma and shows potential therapeutic relevance against both primary and drug-resistant T-cell acute lymphoblastic leukemia (T-ALL).

Current Status

Rizavasertib's highest global development status remains Preclinical. It is not approved for human use or clinical medical treatment and is sold exclusively by chemical suppliers like MedChemExpress as an analytical reference standard or reagent for qualitative, quantitative, and methodological research (such as HPLC, GC, and mass spectrometry).

PAT

US20030199511 and literature Bioorganic & Medicinal Chemistry 2006, 14, 6832–6846, a method for preparing A-443654 is disclosed, 

PAT

WO-03051366

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2003051366&_cid=P11-MTGMSN-41566-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US40155124&_cid=P11-MTGN0W-48129-1

SIMILAR

EXAMPLE 191

(1R)-1-(1H-Indol-3-ylmethyl)-2-[5-(3-methyl-1H-indazol-5-yl)-pyridin-3-yloxy]-ethylamine

MS (ESI) m/e 398 (M+H)+; 1H NMR (300 MHz, DMSO-D6) δ ppm 2.55 (s, 3 H) 3.16 (m, 2 H) 3.86 (d, J=1.70 Hz, 1 H) 4.19 (dd, J=10.51, 6.10 Hz, 1 H) 4.36 (dd, J=10.85, 3.39 Hz, 1 H) 7.01 (t, J=7.46 Hz, 1 H) 7.10 (t, J=6.95 Hz, 1 H) 7.30 (d, J=2.37 Hz, 1 H) 7.38 (d, J=8.14 Hz, 1 H) 7.65 (m, 5 H) 8.07 (s, 1 H) 8.16 (s, 2 H) 8.33 (d, J=2.71 Hz, 1 H) 8.63 (d, J=1.70 Hz, 1 H) 11.04 (bs, 1 H); Anal. Calcd for C24H23N5O.2.9 TFA: C, 49.16; H, 3.59; N, 9.62. Found: C, 49.36; H, 3.66; N, 9.78.

PAT

CN104610229

https://patentscope.wipo.int/search/en/detail.jsf?docId=CN133679262&_cid=P11-MTGNFX-58461-1

Example 4: Preparation of Compound 6

Compound 5 (104 g, 178.9 mmol) and methanol (620 ml, 6V) were added to a 1 L three-necked flask. A 4M HCl/ethyl acetate (130 ml) solution was added dropwise at a temperature below 25 °C. The reaction was allowed to proceed overnight. The reaction was monitored by TLC until the starting material was completely reacted. The mixture was concentrated and drained to dryness using an oil pump to obtain 104 g of crude product. Water (900 ml) and ethyl acetate (1350 ml) were added, and the mixture was stirred until the system was clear. The mixture was allowed to stand, and the organic layer was separated. The aqueous phase was extracted once again with ethyl acetate (500 ml). The organic phases were combined, and water (180 ml) was added. Most of the ethyl acetate was concentrated until solid began to precipitate. The mixture was cooled in an ice bath, stirred, and allowed to crystallize for 30 min. The mixture was filtered, and the filter cake was dried to obtain a white solid (57.9 g, yield 86%, purity 98.3%).

1H NMR(CD 3 OD,500MHz):δppm 8.45(s,1H),8.25(brs,1H),7.98(s,1H),7.61(m,4H),7.37(s,1H),7.16(s,1H),7.10(m,1H),7.00(m,1H),4.18(m,1H),4.03(m,1H),3.56(m,1H),3.10(m,1H),3.00(m,1H),2.62(s,3H)；ESI/MS:m/z＝398(M+H)+.

Pat

• Kinase inhibitorsPublication Number:US-6831175-B2Priority Date:2001-12-13Grant Date:2004-12-14
• 3- (Phenyl-alkoxy) -5- (phenyl) -pyridine derivatives and related compounds as kinase inhibitors for cancer treatmentPublication Number:JP-2005516927-APriority Date:2001-12-13
• Methods of treating muscular wasting diseases using NF-KB activation inhibitorsPublication Number:US-9173920-B2Priority Date:2006-03-15Grant Date:2015-11-03
• Kinase inhibitorsPublication Number:US-2003187026-A1Priority Date:2001-12-13
• 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:CA-2470214-A1Priority Date:2001-12-13
• Kinase inhibitorsPublication Number:US-2003199511-A1Priority Date:2001-12-13
• 3-(phenyl-alkoxy)-5-(phenyl)-pyridine derivatives and related compounds as kinase inhibitors for the treatment of cancerPublication Number:WO-03051366-A2Priority Date:2001-12-13

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References

1.  "Research programme: protein kinase inhibitors - AbbVie". AdisInsight. Springer Nature Switzerland AG.
2.  Luo Y, Shoemaker AR, Liu X, Woods KW, Thomas SA, de Jong R, et al. (June 2005). "Potent and selective inhibitors of Akt kinases slow the progress of tumors in vivo". Molecular Cancer Therapeutics. 4 (6): 977–986. doi:10.1158/1535-7163.MCT-05-0005. PMID 15956255.
3.  Gandelman M, Dansithong W, Kales SC, Paul S, Maag G, Aoyama E, et al. (October 2021). "The AKT modulator A-443654 reduces α-synuclein expression and normalizes ER stress and autophagy". The Journal of Biological Chemistry. 297 (4) 101191. doi:10.1016/j.jbc.2021.101191. PMC 8482485. PMID 34520759.
4.  Ming J, Jin S, Liu Z, Yang K, Shi M, Niu Y (October 2025). "Imidacloprid contributes to bladder cancer progression: preliminary evidence based on network toxicology, machine learning and molecular docking". BMC Pharmacology & Toxicology. 26 (1) 180. doi:10.1186/s40360-025-01016-9. PMC 12577002. PMID 41168844.
5.  Crowell JA, Steele VE, Fay JR (August 2007). "Targeting the AKT protein kinase for cancer chemoprevention". Molecular Cancer Therapeutics. 6 (8): 2139–2148. doi:10.1158/1535-7163.MCT-07-0120. PMID 17699713.
6.  Garcia-Echeverria C, Sellers WR (September 2008). "Drug discovery approaches targeting the PI3K/Akt pathway in cancer". Oncogene. 27 (41): 5511–5526. doi:10.1038/onc.2008.246. PMID 18794885.

Clinical data
Other names	A-443654
Identifiers
IUPAC name
CAS Number	552325-16-3
PubChem CID	10172943
IUPHAR/BPS	8204
DrugBank	DB08073
ChemSpider	8348448
UNII	Q4UG565ZYH
ChEBI	CHEBI:91351
ChEMBL	ChEMBL379300
PDB ligand	L20 (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID20436347
Chemical and physical data
Formula	C24H23N5O
Molar mass	397.482 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

/////////rizavasertib, anax labs, serine/threonine kinase inhibitor, A-443654, A 443654, A443654, Q4UG565ZYH

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Rusfertide

 

Rusfertide

MF
C₁₁₄H₁₈₁N₂₇O₂₈S₂ MW 2442.0 g/mol

isovaleryl-Asp-Thr-His-Phe-Pro-Cys(1)-Ile-Lys(2)-Phe-Glu-Pro-Arg-Ser-Lys-Gly-Cys(1)-Lys-NH2.palmitoyl-Glu(2)-OH

(2S)-5-[4-[(3S,6S,9S,12S,15R,20R,26S,29S,32S,35S)-26-(4-aminobutyl)-6-benzyl-12-[(2S)-butan-2-yl]-32-(3-carbamimidamidopropyl)-3-(2-carboxyethyl)-15-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-3-carboxy-2-(3-methylbutanoylamino)propanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-imidazol-4-yl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]amino]-20-[[(2S)-1,6-diamino-1-oxohexan-2-yl]carbamoyl]-29-(hydroxymethyl)-2,5,8,11,14,22,25,28,31,34-decaoxo-17,18-dithia-1,4,7,10,13,21,24,27,30,33-decazabicyclo[33.3.0]octatriacontan-9-yl]butylamino]-2-(hexadecanoylamino)-5-oxopentanoic acid

{Asp(N-(3-methyl-1-oxobutyl))}-Thr-His-Phe-Pro-Cys-Ile-{Lys(γGlu-C16 acid)}-Phe-Glu-Pro-Arg-Ser-Lys-Gly-Cys-Lys-NH2 (disulfide bridge: Cys6-Cys16)

Mimrylo, APPROVALS 2026, FDA 2026, XM71MYX0IQ, PTG-300FB, PTG-300, TAK 121,

To treat erythrocytosis in adults with polycythemia vera

Rusfertide is a peptide mimetic of natural hepcidin, which targets and degrades ferroportin, reduces serum iron and transferrin-saturation, and thus regulates the production of red blood cells. Rusfertide ameliorates the polycythemia vera, β-thalassemia and hereditary hemochromatosis.

Rusfertide is an injectable peptide mimetic of hepcidin (hepcidin antimicrobial peptide; HAMP; putative liver tumor regressor; PLTR; liver-expressed antimicrobial peptide 1; LEAP-1) with potential use in the treatment of iron deficiency anemia and iron overload secondary to hematologic disorders. Upon administration, rusfertide mimics endogenous hepcidin, a protein primarily produced in hepatocytes, and increases hepcidin levels. As hepcidin plays a key role in the homeostasis of systemic iron, rusfertide may serve to normalize iron levels. Low levels of endogenous hepcidin are associated with iron overload secondary to excessive absorption of iron as seen in beta thalassemia and paradoxically with iron deficiency anemia.

Rusfertide, sold under the brand name Mimrylo, is a medication developed by Protagonist Therapeutics in partnership with Takeda for the treatment of polycythemia vera (PV).^[1][2][3]

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References

Clinical data
Trade names	Mimrylo
Other names	PTG-300; TAK-121
Identifiers
CAS Number	1628323-80-7
PubChem CID	155884410
DrugBank	DB17724
ChemSpider	129955617
UNII	XM71MYX0IQ
KEGG	D12064
ChEMBL	ChEMBL4650507
Chemical and physical data
Formula	C114H181N27O28S2
Molar mass	2441.98 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

References

1.  "Rusfertide - Protagonist Therapeutics". AdisInsight. Springer Nature Switzerland AG.
2.  Kremyanskaya M, Ginzburg YZ, Hoffman R (March 2026). "Modulators of the hepcidin pathway in polycythemia vera and myelofibrosis". Blood. 147 (12): 1278–1288. doi:10.1182/blood.2025028643. PMID 41100735.
3.  "Protagonist and Takeda Announce ASCO Plenary Presentation Highlighting Full 32-Week Results from Phase 3 VERIFY Study of Rusfertide, Showing Reductions in Phlebotomy, Improved Hematocrit Control in Polycythemia Vera". Takeda.

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