Sonrotoclax

CAS 2383086-06-2

MW 890.1 g/mol, MFC₄₉H₅₉N₇O₇S

FDA APPROVED 5/13/2026, Beqalzi, APPROVALS 2026, BGB-11417, BGB 11417, 30R67U9KYS

N-[4-[(4-hydroxy-4-methylcyclohexyl)methylamino]-3-nitrophenyl]sulfonyl-4-[2-[(2S)-2-(2-propan-2-ylphenyl)pyrrolidin-1-yl]-7-azaspiro[3.5]nonan-7-yl]-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide

• 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide
• 2-((1H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-(((trans-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide

To treat adults with relapsed or refractory mantle cell lymphoma after at least two lines of systemic therapy, including a Bruton’s tyrosine kinase inhibitor

Sonrotoclax is a potent, orally active Bcl2 inhibitor. Sonrotoclax has effective cell killing effect against a variety of lymphoma and leukemia cell lines.

Regulatory Status & Primary Indication

On May 13, 2026, the U.S. Food and Drug Administration (FDA) granted accelerated approval to sonrotoclax for treating adult patients with relapsed or refractory mantle cell lymphoma (MCL). [1]

• Eligibility Requirement: Patients must have undergone at least two prior lines of systemic therapy, which must include a Bruton’s tyrosine kinase (BTK) inhibitor.
• Clinical Performance: In the supporting Phase 1/2 BGB-11417-201 trial, sonrotoclax demonstrated an overall response rate (ORR) of 52% and a median time to response of 1.9 months

Sonrotoclax is an orally bioavailable inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon oral administration, sonrotoclax specifically binds to and inhibits the activity of the pro-survival protein Bcl-2. This restores apoptotic processes and inhibits cell proliferation in Bcl-2-overexpressing tumor cells. Bcl-2, a protein that belongs to the Bcl-2 family, is overexpressed in various tumor cell types and plays an important role in the negative regulation of apoptosis. Its tumor expression is associated with increased drug resistance and cancer cell survival.

Sonrotoclax is an investigational new drug that is being evaluated for the treatment of hematologic malignancies, particularly chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL).^[1] It is a potent and selective BCL2 inhibitor that can overcome resistance associated with BCL2 mutations, such as the G101V variant, which limits the effectiveness of first-generation inhibitors like venetoclax.^[2]

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US465731236&_cid=P10-MP4V9K-27469-1

2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide (hereinafter sonrotoclax).

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US335022833&_cid=P10-MP4V1B-17703-1

2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide

Step 9: 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide

A mixture of (S)-2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(2-(2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzoic acid (44 g, 78 mmol), 4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrobenzenesulfonamide (26.8 g, 78 mmol), TFA (15.7 g, 156 mmol), EDCl (19.4 g, 101 mmol) and DMAP (19 g, 156 mmol) in anhydrous DCM (880 mL) was stirred overnight at room temperature. The reaction was monitored by HPLC. After starting material of (S)-2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(2-(2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzoic acid was consumed completely, the reaction mixture was heated to ˜35° C. and N 1,N 1-dimethylethane-1,2-diamine (17.2 g, 195 mmol) was added in one portion. The reaction was stirred for another 12 hours. The mixture was washed twice with 10 wt % aq. AcOH solution (300 mL×2) and then washed with saturated aq. NaHCO 3 (300 mL×2). The organic layer was collected and concentrated to about 90 mL. 22 g of silica gel was added and stirred for 2 hours. After filtration, 180 mL EA was added into the filtrate at reflux and further stirred for 5 hours. After the mixture was cooled to room temperature, the precipitate was filtered and then the wet cake was washed twice with EA (180 mL). After drying in vacuum at 80-90° C., the desired compound was obtained (48 g, yield: 69.5%). 1H NMR (DMSO-d 6) δ ppm: 11.65 (s, 1H), 11.11 (br, 1H), 8.58-8.39 (m, 2H), 8.00 (d, J=2.8 Hz, 1H), 7.74 (d, J=8.8 Hz, 1H), 7.57-7.37 (m, 4H), 7.30-7.10 (m, 3H), 7.00 (d, J=9.2 Hz, 1H), 6.65 (d, J=1.2 Hz, 1H), 6.35 (s, 1H), 6.17 (s, 1H), 4.24 (s, 1H), 3.39-3.20 (m, 5H), 3.04-2.88 (m, 4H), 2.23 (s, 1H), 1.94-1.47 (m, 11H), 1.44-1.26 (m, 7H), 1.19 (d, J=8.0 Hz, 3H), 1.14 (d, J=8.0 Hz, 3H), 1.10 (s, 4H). MS (ESI, m/e) [M+1] + 889.9.

SYN

• US11420968
• https://patentscope.wipo.int/search/en/detail.jsf?docId=US335022833&_cid=P10-MP4VD4-31735-1

Example F43: 2-((1H-pyrrolo[2,3-b]pyridin-5-yl)oxy)-N-((4-((((1r,4r)-4-hydroxy-4-methylcyclohexyl)methyl)amino)-3-nitrophenyl)sulfonyl)-4-(2-((S)-2-(2-isopropylphenyl)pyrrolidin-1-yl)-7-azaspiro[3.5]nonan-7-yl)benzamide

PAT

• Ketal Protected Intermediate for Sonrotoclax and Preparation Method ThereofPublication Number: US-2025320207-A1Priority Date: 2022-12-27
• Methods of treating multiple myeloma using bcl-2 inhibitorPublication Number: US-2025161279-A1Priority Date: 2022-07-21
• Methods of treating myeloid malignancies using bcl-2 inhibitorPublication Number: WO-2023218410-A1Priority Date: 2022-05-12
• Methods of treating myeloid malignancies using bcl-2 inhibitorPublication Number: US-2025057821-A1Priority Date: 2022-05-12
• Methods of treating myeloid malignancies using bcl-2 inhibitorPublication Number: EP-4522169-A1Priority Date: 2022-05-12
• Methods of cancer treatment using bcl-2 inhibitorPublication Number: WO-2021110102-A1Priority Date: 2019-12-02
• Bcl-2 inhibitorsPublication Number: US-2022402915-A1Priority Date: 2018-04-29
• Bcl-2 inhibitorsPublication Number: US-11420968-B2Priority Date: 2018-04-29Grant Date: 2022-08-23
• Bcl-2 inhibitorsPublication Number: US-2021269433-A1Priority Date: 2018-04-29
• Bcl-2 InhibitorsPublication Number: US-2024376104-A1Priority Date: 2018-04-29
• Bcl-2 inhibitorsPublication Number: EP-3788042-B1Priority Date: 2018-04-29Grant Date: 2025-02-12
• Bcl-2 inhibitorsPublication Number: EP-4545515-A1Priority Date: 2018-04-29

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References

References

1.  “Sonrotoclax – BeiGene”. AdisInsight. Springer Nature Switzerland AG.
2.  Tomkins O, D’Sa S (2024). “Review of BCL2 inhibitors for the treatment of Waldenström’s macroglobulinaemia and non-IgM lymphoplasmacytic lymphoma”. Frontiers in Oncology. 14 1490202. doi:10.3389/fonc.2024.1490202. PMC 11570586. PMID 39558954.

Clinical data
Pronunciation	/sɒnˈroʊtəklæks/ son-ROH-tə-klaks
Identifiers
IUPAC name
CAS Number	2383086-06-2
PubChem CID	149553242
ChemSpider	129309008
UNII	30R67U9KYS
KEGG	D12883
ChEMBL	ChEMBL5314951
Chemical and physical data
Formula	C49H59N7O7S
Molar mass	890.11 g·mol−1
3D model (JSmol)	Interactive image
SMILES
InChI

/////////sonrotoclax, anax labs, FDA 2026, APPROVALS 2026, Beqalzi, BGB-11417, BGB 11417, 30R67U9KYS, accelerated approval