United States Patent 10,959,994: Olutasidenib Type A Solid Form, Capsule, and Oral Dosage-Form Patent Analysis

U.S. Patent 10,959,994 protects oral dosage forms containing Type A olutasidenib, the active ingredient in Rezlidhia. Its strongest coverage is directed to the combination of a defined crystalline solid form, specific XRPD and DSC characteristics, and a capsule formulation using microcrystalline cellulose, croscarmellose sodium, and magnesium stearate. The patent does not primarily protect olutasidenib’s molecular structure, therapeutic use, or manufacturing process.

The commercial formulation claims are narrow enough to invite design-around strategies, but the solid-form claims create a meaningful barrier where a generic uses Type A olutasidenib or reproduces the claimed XRPD and thermal profile.

What does U.S. Patent 10,959,994 protect?

U.S. Patent 10,959,994 covers oral unit dosage forms containing Type A olutasidenib. The compound is chemically identified in the claims as:

(S)-5-((1-(6-chloro-2-oxo-1,2-dihydroquinolin-3-yl)ethyl)amino)-1-methyl-6-oxo-1,6-dihydropyridine-2-carbonitrile.

The patent’s protection falls into four principal categories:

Protection category	Representative claims	Scope
Type A solid form plus excipients	1-3, 16-20	Oral dosage forms containing Type A olutasidenib
XRPD-defined solid form	4-8	Dosage forms containing 50-150 mg of a solid form with specified diffraction peaks
Thermal and moisture characteristics	9-10	Type A material characterized by a DSC event at about 256.6°C and DVS water uptake of 0.25% w/w
Commercial dosage composition	11-15, 21-32	50 mg and 150 mg capsules or tablets, including specified excipients and ratios

The claims are composition-of-matter claims directed to dosage forms, not claims to olutasidenib as a chemical compound. A party may avoid infringement by using a different solid form, a different salt or solvate, a different dosage-form architecture, or a formulation that does not satisfy the claimed structural and compositional limitations.

What is the legal status and ownership of U.S. Patent 10,959,994?

U.S. Patent 10,959,994 was issued by the U.S. Patent and Trademark Office for oral dosage forms comprising olutasidenib solid forms. The patent originated with Forma Therapeutics, the developer of olutasidenib. Forma was acquired by Novo Nordisk in 2022, making Novo Nordisk the relevant commercial successor for the olutasidenib program.[1][2]

The patent has a priority chain associated with development of olutasidenib solid forms and oral dosage compositions. The effective patent term is expected to extend into approximately 2038, subject to the actual earliest nonprovisional priority date, patent-term adjustment, terminal disclaimers, and any applicable regulatory patent-term extension.[1]

Item	Assessment
Patent	U.S. 10,959,994
Subject matter	Oral dosage forms containing Type A olutasidenib
Original developer	Forma Therapeutics
Current commercial successor	Novo Nordisk
Patent type	Formulation and solid-form patent
Product association	Rezlidhia, olutasidenib capsules
Expected nominal term	Approximately 2038, subject to USPTO term calculation
Regulatory exclusivity	Separate from patent term; FDA orphan and new-chemical-entity exclusivity apply independently

The precise expiration date should be taken from the USPTO patent-term record and the FDA Orange Book listing, rather than inferred solely from the issue date.[1][3]

How broad are the independent claims?

Claim 1: Type A form plus excipient class

Claim 1 requires:

An oral unit dosage form;
An API consisting essentially of Type A olutasidenib;
A DSC endothermic event at about 256.6°C; and
At least one excipient selected from filler, disintegrant, lubricant, or glidant.

The phrase “consisting essentially of” is important. It generally permits components that do not materially affect the basic and novel characteristics of the claimed Type A formulation, but it does not create unlimited coverage over every olutasidenib dosage form. The claim is broader than the later claims because it does not require a specific dose, capsule size, excipient ratio, or complete XRPD pattern.

A generic capsule containing Type A olutasidenib and conventional excipients could fall within claim 1 even if it does not copy the commercial 50 mg or 150 mg formulation.

Claim 3: Specific excipient group

Claim 3 requires Type A olutasidenib together with one or more of:

Microcrystalline cellulose;
Croscarmellose sodium; or
Magnesium stearate.

This claim narrows the excipient universe but corresponds closely to the commercial formulation. A capsule using all three ingredients would face a substantial claim-mapping risk if the active material is Type A.

Claim 20: Broad Type A dosage-form claim

Claim 20 requires a unit dosage form comprising Type A olutasidenib and one or more excipients. It does not expressly require the DSC event, a specific dose, or a specific excipient combination in the independent claim.

This is potentially the broadest practical claim in the patent because it captures tablets, capsules, and other unit dosage forms containing Type A material. Claims 21-32 narrow that coverage by dose, dosage form, excipient type, micronization, and composition.

What solid form does the patent claim?

The Type A solid form is defined through analytical characteristics rather than only by name. The principal identifiers are:

Analytical method	Claimed characteristic
DSC	Endothermic event at about 256.6°C
XRPD	Peaks at 6.3°, 12.8°, 13.8°, 23.6°, and 27.8° 2θ ±0.2°
Expanded XRPD	Additional peaks at 5.7°, 8.5°, 10.6°, 17.3°, 22.0°, and 22.8°
DVS	Maximum water uptake of 0.25% w/w at 25°C and 90% relative humidity

Claims 4-8 use XRPD to define the solid form. Claim 8 recites a long peak list extending from 5.7° through 38.1° 2θ. The long list can strengthen identification of the intended polymorph but can also create litigation issues concerning peak intensity, sample preparation, instrument calibration, preferred orientation, and acceptable analytical variation.

Claims 9 and 10 provide alternative or additional characterization through DSC and DVS. A product may satisfy one analytical limitation without satisfying every other limitation. In an infringement analysis, the relevant question is whether the accused product contains the claimed solid form and meets the limitations of the asserted claim, not whether its analytical profile is identical in every respect to the patent example.

Which claims protect the marketed Rezlidhia formulation?

The marketed formulation is most closely aligned with claims 11-15 and 29-32.

Claim 15 recites a capsule composition with the following relative weights:

Component	Relative weight
Type A micronized olutasidenib	33.00
Microcrystalline cellulose, Avicel PH101	61.12
Croscarmellose sodium	4.95
Magnesium stearate	1.00
Capsule shell	Size 2 or size 00

Claim 13 recites an approximate 61:5:1 weight ratio for microcrystalline cellulose, croscarmellose sodium, and magnesium stearate. Claim 14 places the active ingredient and excipients at an approximate 33:67 ratio.

The formulation claims create layered protection:

Claims 1 and 20 cover Type A olutasidenib with broad excipient categories.
Claims 3 and 29 cover the principal commercial excipient set.
Claims 11, 12, 21, 22, and 25 cover 50 mg and 150 mg dosage strengths.
Claim 15 covers the detailed commercial composition.
Claims 30-32 address micronized olutasidenib and tablet compositions.

How does the patent compare with a generic launch scenario?

A generic developer would normally evaluate several possible formulation strategies.

Generic strategy	Risk under U.S. 10,959,994
Use the same Type A polymorph	High risk if dosage-form and excipient limitations are met
Use Type A with microcrystalline cellulose, croscarmellose sodium, and magnesium stearate	High risk under claims 3, 16, 20, and 29
Copy the 50 mg or 150 mg capsule composition	Very high risk under claims 11-15
Use a different polymorph with a different XRPD pattern	Lower risk under the solid-form limitations, subject to claim construction
Use a salt, solvate, amorphous form, or co-crystal	Potentially lower risk, depending on whether it qualifies as the claimed Type A form
Use a different excipient system	May avoid narrower excipient claims but not necessarily claims 1 or 20
Use a liquid, suspension, or non-unit dosage form	Potentially outside the asserted dosage-form claims
Use a tablet instead of a capsule	Not necessarily a design-around because claims 20-32 expressly cover tablets

The most effective design-around would usually involve a non-Type A solid form or a materially different chemical form, rather than merely changing the capsule shell or replacing one conventional excipient.

What is the Orange Book status of U.S. Patent 10,959,994?

Rezlidhia was approved by the FDA in December 2022 for adults with relapsed or refractory acute myeloid leukemia having a susceptible IDH1 mutation.[4] FDA-approved olutasidenib is marketed as a 150 mg capsule taken twice daily.[4]

The FDA Orange Book is the controlling source for determining whether U.S. Patent 10,959,994 is listed against Rezlidhia, the listed patent-use code, and the patent expiration date.[3] A formulation patent listed in the Orange Book can create an ANDA certification issue even when the generic applicant does not seek approval for a different clinical use.

For a Paragraph IV challenge, a generic applicant would need to address the listed patent by asserting that:

The patent is invalid;
The patent is unenforceable; or
The proposed product does not infringe.

If the patent is listed and the NDA holder receives a proper Paragraph IV notice, the filing of a patent-infringement action within the statutory period can trigger a 30-month FDA approval stay under the Hatch-Waxman framework.[5]

When does olutasidenib lose regulatory exclusivity?

Olutasidenib received FDA approval as a new chemical entity and for an orphan indication. FDA regulatory exclusivity and patent protection operate independently.

Protection	General effect
New chemical entity exclusivity	Restricts certain ANDA submissions for five years from approval, subject to a Paragraph IV exception
Orphan-drug exclusivity	Restricts approval of the same drug for the same orphan indication for seven years
Patent protection	Depends on the expiration of listed patents and any litigation or settlement
Pediatric exclusivity	Applies only if separately granted by FDA

The FDA approval date was December 1, 2022. On that basis, five-year NCE exclusivity would generally run to December 1, 2027, while seven-year orphan exclusivity would generally run to December 1, 2029, subject to FDA’s official exclusivity coding and any statutory adjustments.[4][6]

The patent may extend beyond those regulatory periods. A generic could therefore face a transition from regulatory blockage to patent-based litigation risk rather than an immediate launch opportunity when NCE exclusivity expires.

Are biosimilar risks relevant to olutasidenib?

No. Olutasidenib is a small-molecule drug, not a biologic. The relevant competitive pathway is an ANDA for a chemically equivalent generic, not a biosimilar application under the Public Health Service Act.

The main competitive issues are:

Polymorph selection;
XRPD and DSC characterization;
Bioequivalence;
Dosage-form composition;
Paragraph IV certification;
Patent litigation;
Potential settlement restrictions.

A generic applicant does not need to reproduce the branded product’s exact formulation if it can demonstrate pharmaceutical equivalence and bioequivalence with a noninfringing formulation.

What manufacturing and intellectual-property barriers remain?

The patent does not claim every manufacturing step for olutasidenib. Its practical manufacturing relevance arises from the need to produce and preserve Type A material in a reproducible form.

Key technical barriers include:

Controlling crystallization conditions to obtain Type A rather than another polymorph.
Preserving the XRPD profile during micronization and blending.
Controlling moisture exposure, despite the claimed low DVS uptake.
Maintaining dose uniformity at 50 mg and 150 mg strengths.
Demonstrating that processing does not convert Type A into another solid form.
Establishing bioequivalence for a formulation with different excipients or particle-size distribution.

A generic company can potentially avoid the patent by developing a different polymorph. That strategy introduces separate regulatory and technical risks, including polymorphic conversion, dissolution changes, stability differences, and the need to demonstrate consistent performance.

How strong is the patent estate for olutasidenib?

The estate represented by U.S. 10,959,994 is strongest against a generic that copies the branded solid form and capsule formulation. It is weaker against a product using a different polymorph, salt, solvate, or nonconforming excipient system.

Factor	Strength assessment
Product-specific protection	Strong
Protection of Type A olutasidenib	Strong if analytical identity is established
Protection of exact commercial capsule	Strong
Protection against alternative polymorphs	Limited
Protection against different dosage forms	Mixed; tablets are expressly covered in later claims
Manufacturing-process coverage	Limited based on the supplied claims
Paragraph IV vulnerability	Dependent on claim construction, validity, and the generic’s solid-form evidence
Biosimilar exposure	Not applicable

Potential validity issues could include written description, enablement, indefiniteness of “about,” analytical reproducibility, anticipation by earlier solid-form disclosures, and obviousness based on polymorph screening. The long XRPD limitation in claim 8 may create evidentiary disputes but also provides a detailed fingerprint for infringement analysis.

What patent litigation and settlement risks affect generic entry?

The supplied claim set does not identify a filed Paragraph IV case, a court docket, or a settlement agreement. The primary litigation trigger would be an ANDA applicant’s Paragraph IV certification against an Orange Book-listed formulation or solid-form patent.

The likely dispute would focus on:

Whether the ANDA product contains Type A olutasidenib;
Whether the accused material exhibits the claimed XRPD or DSC profile;
Whether the claim requires all listed peaks or only the specified diagnostic peaks;
Whether a different polymorph converts to Type A during manufacture or storage;
Whether the formulation meets the claimed weight ratios;
Whether “about” permits the accused composition’s actual values.

A settlement could establish a licensed launch date before patent expiry, but no settlement terms should be inferred without a public court filing or company disclosure.

Key Takeaways

U.S. Patent 10,959,994 is a formulation and solid-form patent for oral olutasidenib dosage forms.
The patent centers on Type A olutasidenib, identified by XRPD, DSC, and DVS characteristics.
Claims 11-15 most closely track the commercial 50 mg and 150 mg capsule composition.
Claims 1 and 20 provide broader coverage than the detailed commercial formulation claims.
A generic using the same Type A material and conventional excipient system faces substantial infringement risk.
A different polymorph, salt, solvate, or formulation may provide a viable design-around, but it would require separate regulatory and pharmaceutical-development work.
Olutasidenib is subject to small-molecule generic competition, not biosimilar competition.
FDA approval occurred December 1, 2022. NCE exclusivity would generally extend to 2027, and orphan exclusivity would generally extend to 2029, subject to FDA’s official records.
The patent is expected to provide protection into approximately 2038, subject to the official USPTO and Orange Book term records.
Paragraph IV litigation risk is concentrated on solid-form identity, XRPD/DSC interpretation, and whether a proposed formulation meets the excipient and dosage-form limitations.

FAQs

Can a generic use olutasidenib without infringing U.S. Patent 10,959,994?

Yes, potentially. A generic may avoid infringement by using a non-Type A solid form or a formulation that does not meet the relevant excipient, dose, or analytical limitations. The final determination depends on the product’s actual solid form and claim construction.

Does changing the capsule shell avoid the patent?

Usually not by itself. The claims focus primarily on the active solid form and formulation components. Claims 11-15 identify capsule compositions, but claims 1, 3, and 20 are not limited solely to a particular capsule shell.

Does the patent cover olutasidenib tablets?

Yes. Claims 23, 26, and 31 expressly identify tablets at 50 mg or 150 mg strengths. Claims 20 and 21 also provide broader unit-dosage-form coverage.

Is Type A olutasidenib the same as the active ingredient in Rezlidhia?

The claims identify Type A olutasidenib as the solid form used in the dosage form. Rezlidhia is FDA-approved as olutasidenib capsules containing 150 mg of active ingredient. The commercial product’s exact solid-form and formulation relationship should be evaluated against the approved labeling and Orange Book records.

Can a generic challenge the patent before 2029?

A Paragraph IV certification can be filed within the Hatch-Waxman framework subject to statutory timing rules. Regulatory exclusivity, patent listing, FDA submission timing, and any resulting litigation determine whether approval or launch can occur before the end of orphan exclusivity.

References

United States Patent and Trademark Office. (2021). U.S. Patent No. 10,959,994, oral dosage forms comprising solid forms of olutasidenib.
Novo Nordisk A/S. (2022). Annual report 2022.
U.S. Food and Drug Administration. (n.d.). Approved drug products with therapeutic equivalence evaluations: Orange Book.
U.S. Food and Drug Administration. (2022, December 1). FDA approves olutasidenib for relapsed or refractory acute myeloid leukemia with a susceptible IDH1 mutation.
Drug Price Competition and Patent Term Restoration Act of 1984, 21 U.S.C. § 355(j).
U.S. Food and Drug Administration. (n.d.). Regulatory exclusivity provisions and patent certifications under the Hatch-Waxman Amendments.

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Rigel Pharms	REZLIDHIA	olutasidenib	CAPSULE;ORAL	215814-001	Dec 1, 2022		RX	Yes	Yes	10,959,994	⤷ Start Trial	Y				⤷ Start Trial
>Applicant	>Tradename	>Generic Name	>Dosage	>NDA	>Approval Date	>TE	>Type	>RLD	>RS	>Patent No.	>Patent Expiration	>Product	>Substance	>Delist Req.	>Patented / Exclusive Use	>Submissiondate

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Denmark	3720442	⤷ Start Trial
European Patent Office	3720442	⤷ Start Trial
European Patent Office	4215197	⤷ Start Trial
Spain	2941079	⤷ Start Trial
>Country	>Patent Number	>Estimated Expiration	>Supplementary Protection Certificate	>SPC Country	>SPC Expiration

Details for Patent: 10,959,994

Which drugs does patent 10,959,994 protect, and when does it expire?

Summary for Patent: 10,959,994