Revumenib is a first-in-class, orally active menin inhibitor developed for the treatment of genetically defined acute leukemias. It inhibits the interaction between menin and KMT2A-associated proteins, disrupting transcriptional programs involved in leukemia development. FDA approved Revuforj (revumenib) in November 2024 for relapsed or refractory acute leukemia with a KMT2A translocation, and in October 2025 expanded the indication to relapsed or refractory AML with a susceptible NPM1 mutation.
The Revumenib free base has CAS Number 2169919-21-3, molecular formula C32H47FN6O4S, and molecular weight 630.82 g/mol.
The marketed pharmaceutical drug substance is revumenib citrate hydrate, also described by FDA as revumenib monocitrate monohydrate. Its molecular formula is C32H47FN6O4S·C6H8O7·H2O and molecular weight is 840.96 g/mol.
Revumenib is a small-molecule menin inhibitor originally developed as SNDX-5613. FDA's quality assessment describes it as a potent, orally available inhibitor of the interaction between menin and KMT2A fusion proteins and wild-type KMT2A.
For the commercial product, the salt form was changed during development to revumenib citrate, specifically the monocitrate monohydrate form. FDA confirms that the commercial drug substance is revumenib citrate and that the final tablets contain 25, 110 and 160 mg strengths expressed as free-base equivalents.
| Parameter | Revumenib |
|---|---|
| Product Name | Revumenib |
| Pharmaceutical Form | Revumenib Citrate Hydrate / Monocitrate Monohydrate |
| Free Base CAS Number | 2169919-21-3 |
| Citrate Hydrate CAS Number | 2761046-45-9 |
| Free Base Formula | C32H47FN6O4S |
| Free Base Molecular Weight | 630.82 g/mol |
| Citrate Hydrate Formula | C38H57FN6O12S |
| Citrate Hydrate Molecular Weight | 840.96 g/mol |
| Therapeutic Class | Antineoplastic |
| Pharmacological Class | Menin inhibitor |
| Development Code | SNDX-5613 |
| Physical Form | White to faint pink solid for citrate hydrate |
| BCS Classification | BCS III |
| Drug Substance Solubility | High |
| Water/Solution Behavior | Highly soluble in relevant pH media |
| Chirality | Contains defined trans cyclohexyl stereochemistry |
FDA reports that revumenib citrate hydrate is a white to faint pink solid and is soluble at pH 1.2 and 6.8, while being sparingly soluble at pH 4.5.
Revumenib is used as a targeted antineoplastic therapy for genetically defined acute leukemia.
Its pharmaceutical applications include:
FDA's current approval covers patients 1 year and older with relapsed or refractory acute leukemia with a KMT2A translocation, and the 2025 approval expanded use to susceptible NPM1-mutated relapsed/refractory AML.
Revumenib citrate API requires control of chemical identity, assay, related substances, salt/hydrate form and solid-state characteristics. FDA's CMC review specifically identifies the commercial drug substance as revumenib monocitrate monohydrate and confirms that incoming drug-substance lots conformed to the proposed commercial drug-substance specifications.
FDA also notes that the correct API polymorphic form is included as part of the proposed drug-substance quality-control specifications.
Relevant analytical techniques can include:
Current research-grade analytical material for free-base Revumenib has been reported at 99.98% assay/purity by MedChemExpress; this is a commercial analytical value and should not be represented as an official pharmacopoeial release limit.
Revumenib API manufacturing requires careful control of the active pharmaceutical ingredient's chemical purity and pharmaceutical form. FDA's development documentation confirms that the commercial drug substance is the citrate monohydrate salt and that polymorphic-form control is part of the API quality strategy.
A quality-focused manufacturing and analytical program should therefore address:
Revumenib citrate API should be packaged in an appropriate, tightly closed pharmaceutical container with protection against moisture, contamination and unsuitable environmental conditions.
For the finished Revuforj tablets, FDA specifies storage at 20–25°C, with permitted excursions between 15–30°C. This finished-product storage condition should not automatically be treated as the API storage specification.
Typical Revumenib API documentation can include:
Revumenib is a recently approved targeted oncology API with a technically important citrate-hydrate drug-substance form. FDA's CMC assessment specifically addresses the commercial citrate drug substance, its high solubility and control of the correct API polymorphic form.
A quality-oriented Revumenib API manufacturing program should emphasize:
| Parameter | Specification |
|---|---|
| Appearance | white to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 98.0% – 102.0% |
| Loss on Drying | NMT 0.5% |
| Residue on Ignition | NMT 0.1% |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 1.0% |
| Water Content | NMT 1.0% |