Details for Patent: 9,593,100

Which drugs does patent 9,593,100 protect, and when does it expire?

Patent 9,593,100 protects BRAFTOVI and is included in one NDA.

This patent has seventy-five patent family members in forty-nine countries.

Summary for Patent: 9,593,100

Title:	Compounds and compositions as protein kinase inhibitors
Abstract:	The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
Inventor(s):	Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
Assignee:	Novartis AG , Array Biopharma Inc
Application Number:	US14/994,827
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,593,100
Patent Claim Types: see list of patent claims	Composition; Compound; Device; Dosage form;

US Patent 9,593,100: Encorafenib Composition Claims, Patent Scope, and Generic Entry Risk

US Patent 9,593,100 covers pharmaceutical compositions and combination products containing encorafenib, the BRAF inhibitor marketed as Braftovi. It does not claim encorafenib as a chemical compound in isolation. Its principal commercial relevance is protection for encorafenib-containing formulations, particularly oral tablets or capsules, and for combinations with MEK inhibitors including binimetinib, formerly identified as ARRY-438162.[1][2]

The patent’s broadest claims require encorafenib, or a pharmaceutically acceptable salt, together with a pharmaceutically acceptable excipient or co-agent. The patent therefore creates formulation and combination-product exposure for competing products even where the underlying encorafenib compound patent has expired or is separately challenged.

What drug does US Patent 9,593,100 protect?

The claimed compound is encorafenib, also known by the development code LGX818. Its systematic name in the patent is:

“Methyl N-[(2S)-1-({4-[3-(5-chloro-2-fluoro-3-methanesulfonamidophenyl)-1-(propan-2-yl)-1H-pyrazol-4-yl]pyrimidin-2-yl}amino)propan-2-yl]carbamate.”

Encorafenib selectively inhibits mutant BRAF kinase, including BRAF V600E and V600K. The FDA approved Braftovi in combination with binimetinib for patients with unresectable or metastatic melanoma containing a BRAF V600E or V600K mutation.[2] The approved uses later expanded to include BRAF V600E-mutated metastatic colorectal cancer in combination with cetuximab after prior therapy.[3]

Commercial product and manufacturer

Item	Information
Brand	Braftovi
Active ingredient	Encorafenib
Development code	LGX818
Initial U.S. approval	2018
Original developer	Array BioPharma Inc.
Current commercial owner	Pfizer Inc. following Pfizer’s acquisition of Array
Dosage form	Oral capsules
Principal melanoma combination	Encorafenib plus binimetinib
CRC combination	Encorafenib plus cetuximab
Drug class	BRAF kinase inhibitor

The listed MEK inhibitor ARRY-438162 is binimetinib, which is marketed as Mektovi. Claims 12, 18, and 19 expressly narrow the combination to encorafenib and binimetinib.

What are the independent claims in US Patent 9,593,100?

The claim set contains two principal independent claim categories.

Claim 1: encorafenib pharmaceutical composition

Claim 1 requires:

1. Encorafenib or a pharmaceutically acceptable salt; and
2. One or more pharmaceutically acceptable excipients.

This is a composition claim. It is broader than a claim limited to a particular tablet, capsule, dose, dissolution profile, crystal form, or excipient concentration.

A product containing encorafenib without an excipient would not meet the literal requirement of claim 1. A conventional finished oral dosage form normally would contain excipients and therefore presents a stronger infringement case than bulk active pharmaceutical ingredient.

Claim 14: encorafenib pharmaceutical combination

Claim 14 requires:

1. Encorafenib or a pharmaceutically acceptable salt; and
2. One or more co-agents.

The claim does not require that the two agents be physically combined in one dosage unit. The later claims expressly cover both fixed and non-fixed combinations, as well as kits.

This structure is important. A two-bottle regimen containing encorafenib and a separate co-agent may fall within the non-fixed combination claims if the product, labeling, packaging, or instructions establish the claimed combination.

How do claims 1 through 25 narrow the patent scope?

Claims	Subject matter	Scope effect
1	Encorafenib or salt plus excipient	Broad composition claim
2	Encorafenib, rather than a salt	Narrows claim 1
3	Oral administration	Excludes non-oral formulations
4	Functional excipient categories	Identifies diluents, binders, lubricants, disintegrants and other excipient classes
5	Specific conventional excipients	Provides a long list of named excipients
6	Tablet or capsule	Targets the principal commercial dosage forms
7	Approximately 1 mg to 500 mg encorafenib	Adds a broad dose range
8	Additional therapeutic agent	Combination composition
9	Additional agent is an anticancer compound	Narrows the combination
10	Additional agent is a MEK inhibitor	Targets BRAF-MEK treatment
11	Listed MEK inhibitors	Defines a closed species list
12	ARRY-438162	Specifically covers binimetinib
13	Encorafenib plus ARRY-438162	Combination composition with the named agents
14	Encorafenib or salt plus co-agent	Broad combination claim
15	Co-agent is an anticancer compound	Narrows claim 14
16	Co-agent is a MEK inhibitor	BRAF-MEK combination
17	Listed MEK inhibitors	Closed list of named MEK inhibitors
18	ARRY-438162	Binimetinib-specific limitation
19	Encorafenib plus ARRY-438162	Specific combination
20	Non-fixed combination	Separate dosage units or administration components
21	Fixed combination	Same dosage form or fixed co-formulation
22	Approximately 1 mg to 500 mg encorafenib	Dose limitation
23	Kit	Packaging-based combination
24	Kit with administration instructions	Adds instructions as a claimed kit element
25	Encorafenib salt	Salt-specific composition claim

Claims 2 through 7 form a nested oral-product series. Claims 8 through 13 address compositions with additional anticancer agents, especially MEK inhibitors. Claims 14 through 25 use a separate “pharmaceutical combination” format and expand the coverage to fixed combinations, non-fixed regimens, and kits.

What formulations are protected by US Patent 9,593,100?

The patent is directed to formulation-level protection rather than a narrowly defined formulation technology.

Claim 6 expressly covers tablets and capsules. Claim 3 covers oral administration without limiting the dosage form. The excipient language in claims 4 and 5 encompasses standard pharmaceutical ingredients, including:

• Lactose, dextrose, sucrose, mannitol, and sorbitol
• Cellulose derivatives and starches
• Silica, talc, stearic acid, and metal stearates
• Polyethylene glycol
• Gelatin, tragacanth, methylcellulose, and polyvinylpyrrolidone
• Sodium carboxymethylcellulose
• Agar and alginic acid salts
• Colorants, flavors, sweeteners, absorbents, lubricants, binders, and disintegrants

The practical coverage is broad because most conventional oral encorafenib products use one or more ingredients within these categories. A generic manufacturer would need to assess both the actual formulation and the formulation disclosed in its ANDA.

Does claim 1 cover Braftovi capsules?

Braftovi is an oral capsule containing encorafenib and inactive ingredients. On the face of the claims, the commercial capsule is the type of product targeted by claims 1, 2, 3, 6, and potentially 7. A definitive infringement analysis would require comparison with the approved product’s qualitative and quantitative composition and the patent’s file history.

What patent expiration date applies to US Patent 9,593,100?

US Patent 9,593,100 was granted on March 14, 2017. Its nominal patent term is generally calculated from the relevant nonprovisional filing date, subject to terminal disclaimers, patent-term adjustment, patent-term extension, and other statutory adjustments.[1][4]

Public patent records identify a nominal expiration in 2034 for this patent family. The precise operative date should be taken from the current USPTO patent record and any applicable FDA Orange Book listing. Patent expiration is distinct from FDA regulatory exclusivity and from the expiration of other patents covering encorafenib, binimetinib, polymorphs, manufacturing processes, or approved methods of use.

Exclusivity layer	Relevance to encorafenib
Compound patent	Protects the encorafenib molecule itself
US 9,593,100	Protects encorafenib compositions and combinations
Formulation patents	May cover specific dosage forms, excipient systems, release properties, or solid states
Method-of-use patents	May cover BRAF-mutant cancer treatment or specific combination regimens
FDA exclusivity	Independent regulatory barrier under the Hatch-Waxman statute
Patent-term extension	May extend an eligible patent based on regulatory review

What is the Orange Book status of US Patent 9,593,100?

Braftovi is an FDA-approved small-molecule drug listed in the Orange Book. The Orange Book may identify patents associated with approved encorafenib indications, dosage forms, and methods of use.[5]

A patent listing does not mean that every claim is necessarily infringed by every generic product. It gives the patent holder a statutory basis to receive notice of an ANDA certification and, if applicable, to bring a patent infringement action within the Hatch-Waxman framework.

The relevant regulatory distinction is:

• Product or formulation claims may be implicated by an ANDA that copies the active ingredient and dosage form.
• Method-of-use claims may be addressed through a section viii statement or a carve-out if the generic label omits the patented use.
• A Paragraph IV certification asserts that the listed patent is invalid, unenforceable, or not infringed.
• A Paragraph III certification accepts delay until patent expiration.

For a capsule product that uses encorafenib with conventional excipients, claims 1, 2, 3, 6, and 7 are more commercially relevant than the combination claims unless the generic label, packaging, or proposed use includes binimetinib or another listed co-agent.

What Paragraph IV challenges could target this patent?

A generic applicant could challenge US 9,593,100 through a Paragraph IV certification on several grounds.

Non-infringement

A generic applicant could argue that its product does not contain:

• Encorafenib in the claimed form
• A pharmaceutically acceptable excipient
• An oral dosage form, where the claim requires oral administration
• A listed MEK inhibitor or other co-agent
• The claimed fixed or non-fixed combination
• A kit containing the required instructions

Claims 14 through 24 may be avoided more readily than claim 1 if the generic product contains only encorafenib and does not promote a combination regimen.

Obviousness

The principal obviousness attack would combine:

1. Prior art disclosing encorafenib;
2. Prior art disclosing conventional oral pharmaceutical excipients;
3. Prior art teaching BRAF-MEK inhibitor combinations; and
4. Prior art disclosing binimetinib or another MEK inhibitor.

The broadness of claims 1 and 14 creates potential obviousness exposure. Conventional excipients and routine tablet or capsule preparation generally provide a predictable formulation rationale. The patent holder would likely rely on formulation performance, stability, bioavailability, safety, or unexpected combination efficacy to defend the claims.

Written description and enablement

The claims extend across:

• Encorafenib salts;
• Multiple excipient classes;
• Oral dosage forms;
• A 1 mg to 500 mg dose range;
• Multiple MEK inhibitors;
• Fixed and non-fixed combinations;
• Kits and administration instructions.

A challenger could argue that the specification does not adequately support the full breadth of every claimed species or enable the full combination and formulation genus without undue experimentation.

Definiteness and claim-construction issues

The terms “about,” “one or more,” “pharmaceutically acceptable,” “co-agents,” and “non-fixed combination” could generate claim-construction disputes. Claim 5 also contains drafting irregularities, including the phrase “an absorbents,” which may affect interpretation but does not automatically invalidate the claim.

How strong is the patent estate for encorafenib?

US 9,593,100 is commercially meaningful but narrower than an encorafenib compound patent.

Factor	Assessment
Direct product coverage	Strong for oral encorafenib formulations containing excipients
Chemical compound coverage	None apparent from the supplied claims
Combination coverage	Strong for encorafenib plus the specifically listed MEK inhibitors
Formulation specificity	Moderate; the claims are broad but not tied to a unique formulation architecture
Salt coverage	Present in claims 1, 14, and 25
Kit coverage	Present in claims 23 and 24
Dose coverage	Broad 1 mg to 500 mg range
Vulnerability to obviousness	Higher for conventional excipient and broad combination claims
Design-around potential	Greater for non-combination generic products than for ordinary oral encorafenib capsules
Biosimilar relevance	None; encorafenib is a small molecule

The patent’s strongest practical feature is the combination of a broad composition claim with explicit oral dosage-form claims. Its weaker feature is the absence, in the supplied claims, of a defined particle size, polymorph, dissolution specification, excipient ratio, manufacturing step, or pharmacokinetic limitation.

What method-of-use and combination patents matter for Braftovi?

The supplied claims are composition and combination claims. They do not independently require treatment of melanoma, colorectal cancer, a BRAF mutation, or a particular dosing schedule.

Separate patent families may cover:

• Treatment of BRAF V600E or V600K tumors
• Encorafenib plus binimetinib
• Encorafenib plus cetuximab
• Specific dosing schedules
• Resistance management
• Solid forms, salts, intermediates, and manufacturing processes
• Pharmaceutical compositions with defined release or stability properties

Those families must be analyzed separately from US 9,593,100. A generic applicant could avoid a method-of-use claim through a label carve-out while still facing a product-composition claim.

Which companies are challenging encorafenib exclusivity?

The supplied claim text identifies no ANDA filer, Paragraph IV notice, district-court action, PTAB proceeding, or settlement agreement. The patent itself does not establish a challenger or litigation status.

The competitive risk comes primarily from generic manufacturers pursuing an encorafenib capsule or tablet through an ANDA. A separate biosimilar pathway is not relevant because encorafenib is a chemically synthesized small molecule, not a biologic.

Potential challengers would evaluate:

• The Orange Book-listed patent set
• The compound patent’s remaining term
• US 9,593,100 and any continuation patents
• Approved indications and label carve-out options
• Binimetinib combination rights
• Manufacturing and solid-form patents
• The commercial value of a standalone encorafenib product

What generic launch scenarios exist for encorafenib?

Launch after all relevant patents expire

This is the lowest-risk pathway if the generic applicant accepts the listed patents and waits for expiration. It preserves litigation certainty but delays market entry.

Paragraph IV launch

A Paragraph IV strategy could challenge US 9,593,100 on invalidity or non-infringement grounds. The highest-value target would be a generic oral encorafenib capsule, while the combination claims may be avoided by omitting binimetinib from the label and product package.

Label carve-out

A generic could seek approval for indications that do not require a patented method of use. This strategy does not necessarily avoid formulation claims, which attach to the product itself.

At-risk launch

An at-risk launch could occur after litigation remains unresolved or after a court decision favorable to the generic. The principal risks include damages, injunction exposure, launch disruption, and separate enforcement of other encorafenib patents.

What revenue exposure does the patent create?

Braftovi revenue is exposed to generic substitution when a legally and commercially viable encorafenib product enters the U.S. market. US 9,593,100 can delay or complicate substitution for conventional oral products because a generic capsule is likely to contain both encorafenib and excipients.

The patent is less likely to block:

• Bulk API sales that do not constitute the claimed pharmaceutical composition
• Products using a non-oral route, subject to claim 1
• Products that omit the claimed co-agent
• Products approved only for uses that can be carved out, where no product claim applies
• Products entering after expiration or successful invalidation

For Pfizer, the material commercial question is not this patent in isolation. It is the combined expiration profile of the compound, composition, formulation, method-of-use, combination, and manufacturing patents associated with Braftovi and Mektovi.

Key Takeaways

• US 9,593,100 covers encorafenib pharmaceutical compositions, not encorafenib as a chemical compound by itself.
• Claims 1 through 7 target oral encorafenib products, including tablets and capsules with conventional excipients.
• Claims 8 through 13 cover encorafenib compositions with anticancer agents, particularly MEK inhibitors.
• Claims 14 through 24 separately cover encorafenib combinations, fixed combinations, non-fixed combinations, and kits.
• ARRY-438162 in claims 12, 18, and 19 is binimetinib.
• The claims extend to pharmaceutically acceptable salts and an encorafenib dose range of approximately 1 mg to 500 mg.
• The patent has a nominal 2034 expiration profile based on public patent records, subject to applicable statutory adjustments.
• Generic encorafenib capsules are the most direct product risk.
• The broad excipient and combination language creates potential obviousness, written-description, enablement, and claim-construction challenges.
• No biosimilar pathway applies.
• The patent’s commercial impact depends on the complete Braftovi patent and Orange Book estate, not US 9,593,100 alone.

FAQs

Does US Patent 9,593,100 claim encorafenib itself?

No. The supplied claims require encorafenib in a pharmaceutical composition or combination. A separate compound patent would provide the principal molecule-level protection.

Does the patent cover encorafenib capsules sold without binimetinib?

The supplied composition claims can cover an encorafenib capsule containing excipients without binimetinib. The combination claims require a co-agent and do not apply to every standalone capsule.

Can a generic avoid the patent by using different excipients?

Changing excipients may not avoid claim 1 because that claim broadly requires one or more pharmaceutically acceptable excipients. It may be more relevant to claim 5, which lists specific excipient categories and ingredients.

Does a kit with separate encorafenib and binimetinib packages fall within the patent?

Claims 23 and 24 expressly address kits containing encorafenib and co-agents with administration instructions. Separate packaging does not necessarily avoid the claims.

Is US Patent 9,593,100 relevant to Braftovi’s colorectal cancer indication?

Potentially, but the supplied claims do not recite colorectal cancer or cetuximab. The patent’s direct relevance to that indication depends on the product and combination claims, while separate method-of-use patents may address the colorectal cancer regimen.

References

1. U.S. Patent No. 9,593,100, “Pharmaceutical compositions comprising a BRAF inhibitor.” U.S. Patent and Trademark Office. (2017).
2. U.S. Food and Drug Administration. (2018). Braftovi (encorafenib) prescribing information.
3. U.S. Food and Drug Administration. (2020). FDA approves encorafenib with cetuximab and binimetinib for metastatic colorectal cancer with a BRAF V600E mutation.
4. U.S. Patent and Trademark Office. (2023). Manual of Patent Examining Procedure, patent term and patent term adjustment provisions.
5. U.S. Food and Drug Administration. (2024). Approved drug products with therapeutic equivalence evaluations: Orange Book.

Drugs Protected by US Patent 9,593,100

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-001	Jun 27, 2018		DISCN	Yes	No			Y
Array Biopharma Inc	BRAFTOVI	encorafenib	CAPSULE;ORAL	210496-002	Jun 27, 2018		RX	Yes	Yes			Y

International Family Members for US Patent 9,593,100

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2470526		PA2019005	Lithuania
European Patent Office	2727918		PA2019006	Lithuania
European Patent Office	2470526		300973	Netherlands