Prosecution Insights
Last updated: April 19, 2026
Application No. 18/028,058

PHARMACEUTICAL FORMULATION

Non-Final OA §103
Filed
Mar 23, 2023
Examiner
LEE, SIN J
Art Unit
1613
Tech Center
1600 — Biotechnology & Organic Chemistry
Assignee
Agios Pharmaceuticals, Inc.
OA Round
1 (Non-Final)
69%
Grant Probability
Favorable
1-2
OA Rounds
3y 0m
To Grant
94%
With Interview

Examiner Intelligence

Grants 69% — above average
69%
Career Allow Rate
716 granted / 1039 resolved
+8.9% vs TC avg
Strong +26% interview lift
Without
With
+25.5%
Interview Lift
resolved cases with interview
Typical timeline
3y 0m
Avg Prosecution
59 currently pending
Career history
1098
Total Applications
across all art units

Statute-Specific Performance

§101
0.3%
-39.7% vs TC avg
§103
46.3%
+6.3% vs TC avg
§102
18.9%
-21.1% vs TC avg
§112
20.2%
-19.8% vs TC avg
Black line = Tech Center average estimate • Based on career data from 1039 resolved cases

Office Action

§103
DETAILED ACTION Notice of Pre-AIA or AIA Status The present application, filed on or after March 16, 2013, is being examined under the first inventor to file provisions of the AIA. Claim Objections Claims 1 and 22 are objected to because of the following informalities: on the second line in each of claims 1 and 22, applicant need to change “and” (located between “cell disease” and “thalassemia”) to --- or ---. Appropriate correction is required. Claim Rejections - 35 USC § 103 This application currently names joint inventors. In considering patentability of the claims the examiner presumes that the subject matter of the various claims was commonly owned as of the effective filing date of the claimed invention(s) absent any evidence to the contrary. Applicant is advised of the obligation under 37 CFR 1.56 to point out the inventor and effective filing dates of each claim that was not commonly owned as of the effective filing date of the later invention in order for the examiner to consider the applicability of 35 U.S.C. 102(b)(2)(C) for any potential 35 U.S.C. 102(a)(2) prior art against the later invention. The following is a quotation of 35 U.S.C. 103 which forms the basis for all obviousness rejections set forth in this Office action: A patent for a claimed invention may not be obtained, notwithstanding that the claimed invention is not identically disclosed as set forth in section 102, if the differences between the claimed invention and the prior art are such that the claimed invention as a whole would have been obvious before the effective filing date of the claimed invention to a person having ordinary skill in the art to which the claimed invention pertains. Patentability shall not be negated by the manner in which the invention was made. The factual inquiries for establishing a background for determining obviousness under 35 U.S.C. 103 are summarized as follows: 1. Determining the scope and contents of the prior art. 2. Ascertaining the differences between the prior art and the claims at issue. 3. Resolving the level of ordinary skill in the pertinent art. 4. Considering objective evidence present in the application indicating obviousness or nonobviousness . Claim (s) 1, 2, 4, 6-8, 10, 12, 14, 15, 17, 20-25 and 56-58 are rejected under 35 U.S.C. 103 as being unpatentable over Sizemore et al (WO 2019/104134 A1) in view of Lee et al (“Sprinkle formulations-A review of commercially available products”, Asian Journal of Pharmaceutical Sciences , vol.15(3) (July 2019), pg.1-19), CDC chart (“2 to 20 years: Boys Stature-for-age and Weight-for-age percentiles” – a chart published on May 30, 2000 and obtained from the website: https://www.cdc.gov/growthcharts/data/set2clinical/cj41c071.pdf ) and Agresta et al (WO 2016/201227 A1) ( with a Wikipedia article on “Capsule (pharmacy)” obtained from the website: https://en.wikipedia.org/wiki/Capsule_(pharmacy) , which is cited here merely to support the Examiner’s assertion that Size 1 Capsule has a volume of 0.48 mL, a length of 19.4 mm and a diameter of 6.91 mm ) . Sizemore teaches (abstract, [0042], [0056] -[ 0059], [0125], [0127]) a method of treating a disease selected from pyruvate kinase deficiency, sickle cell disease or thalassemia , which comprises administering to a subject in need thereof an effective amount of crystalline Form A. Crystalline Form A refers to a hemisulfate sesquihydrate of Compound 1 , and Compound 1 is N-(4-(4-( cyclopropylmethyl )piperazine -l- carbonyl)phenyl)quinoline-8-sulfonamide which structure is shown below: . Thus, Sizemore’s Compound 1 is instant mitapivat (se [0003] of present specification ), and Sizemore’s Crystalline Form A , which is a hemisulfate sesquihydrate of Compound 1 teaches instant mitapivat hemisulfate sesquihydrate ( a pharmaceutically acceptable salt of mitapivat ). Sizemore further teaches ([0053]) that the subject in need of the treatment can refer to a human child no more than 18 years old . Such range for the age overlaps with instant ranges for the age of the pediatric subject of claim 1 (about 1 to 12 years of age), claims 2, 7 and 10 (about 2 years of age to less than about 12 years of age), claim 12 (about 1 year of age to less than about 2 years of age) and claim 22 (about 2 years of age to less than about 12 years of age), thus rendering instant age rages prima facie obvious . In the case “where the [claimed] ranges overlap or lie inside ranges disclosed by the prior art,” a prima facie case of obviousness would exist which may be overcome by a showing of unexpected results, In re Wertheim , 541 F.2d 257, 191 USPQ 90 (CCPA 1976). With respect to instant range for the body weight of the pediatric subject , although Sizemore does not explicitly teach such limitation, CDC chart (“2 to 20 years: Boys Stature-for-age and Weight-for-age percentiles” – a chart published on May 30, 2000 and obtained from the website: https://www.cdc.gov/growthcharts/data/set2clinical/cj41c071.pdf ) indicates that 50 percentile weight for boys aged from 2 to 12 years old ranges from 12 kg to 40 kg . Such weight range indicated by CDC overlaps with instant ranges for the weight of the pediatric subject of claim 1 (about 7 kg to less than about 40 kg), claim 4 (about 7 kg to less than about 20 kg), claim 7 (about 20 kg to less than about 40 kg), claim 10 (about 7 kg to less than about 20 kg) and claim 22 (about 20kg to less than about 40kg) , thus rendering instant weight ranges prima facie obvious . In re Wertheim, supra . With respect to instant limitation of administering mitapivat or its salt together with food or water , although Sizemore does not explicitly teach such limitation, first of all , Agresta teaches (pg.40, lines 6-7) that food has a minimal effect on the exposure to Compound 1 ( instant mitapivat – see pg.4, lines 1-4), which means that it is safe to take mitapivat together with food . Secondly , as evidenced by Lee et al (see both paragraphs under Introduction on pg.1 ; pg.2, left-hand column, 1 st paragraph), it is known in the art that even though dosage forms like capsules and tablets are preferred due to dosing convenience, high physico chemical stability and cost-effectiveness, the large size of sold formulations is challenging for patients with dysphagia (often the elderly and children) to swallow, which in turn promoted the development of sprinkle formulations. Sprinkle formulations are drug containing pellets or granules that can be mixed with soft food before administration. These formulations provide almost the same dosing flexibility and ease of ingestion as liquid formulations when sprinkled on liquid or semi-solid vehicles, such as apple sauce, pudding or yogurt. The food taken together with the drug can also mask the unpleasant taste and smell of the drug substance which potentially improves patient compliance. Since Sizemore teaches ([0219]) that its Crystalline Form A ( instant mitapivat hemisulfate sesquihydrate ) can be formed into a tablet either through dry or wet granulation, it would have been obvious to one skilled in the art to use Sizemore’s Crystalline Form A in granular form (instead of tablet form) and sprinkle it on food before administering to a human child (under age of 18) with a reasonable expectation of making Crystalline Form A easier to swallow fo r children (who usually have dysphagia) and masking any unpleasant taste and smell of Crystalline Form A so as to improve patience compliance. Thus, Sizemore in view of CDC chart, Agresta and Lee renders obvious instant claims 1, 2, 4, 14 and 20 . With respect to the dosage amount claimed in claim 6 (0.5-25 mg), claim 7 (0.5-25 mg), claim 8 ( 15-25 mg, 5-15 mg or 1-5 mg), claim 10 (10-20 mg, 1-20 mg or 0.5-5 mg) and claim 12 (8-12 mg, 2-6 mg or 0.5-3 mg), Sizemore teaches ([00111]) that a specific dosage and treatment regimen for any particular subject will depend upon a variety of factors including age, body weight, general health, sex, diet, time of administration, rate of excretion, drug combination, the judgement of treating physicians and severity of the particular disease. Sizemore further teaches ([00112]) that Crystalline Form A ( instant m itapivat hemisulfate sesquihydrate ) is formulated for administration at a dose equivalent of about 2 mg to about 3000 mg of Compound 1 (instant mitapivat ) . Under such general guideline given by Sizemore, instant ranges for the dosage amounts as claimed in claims 6-8, 10, 12 and 22-25 would have been obvious to one skilled in the art before the effective filing date of the claimed invention since it has been held that where the general conditions of a claim are disclosed in the prior art, discovering the optimum or workable ranges involves only routine skill in the art. In re Aller, 105 USPQ 233 . Thus, Sizemore in view of CDC chart, Agresta and Lee renders obvious instant claims 6-8, 10 and 12. With respect to instant claims 17 and 21 , Sizemore teaches ([00112]) that the dosing may be administered once, twice or three times daily . Thus, S izemore in view of CDC chart, Agresta and Lee renders obvious instant claims 17 and 21. With respect to instant claim 15 , the Examiner established above that it would have been obvious to one skilled in the art to use Sizemore’s Crystalline Form A in granular form (instead of tablet form) and sprinkle it on food before administering to a human child (under age of 18) . As to instant limitation of the one or more granules each comprising about 0.5 mg to about 1.5 mg of mitapivat or its salt , first of all , Sizemore teaches ([00114]) that its tablet formulation contains Crystalline Form A ( mitapivat hemisulfate sesquihydrate ) in an amount equivalent to about 1 to 200 mg of Compound 1 ( mitapivat ). This means that the total amount of mitapivat for all of the granules in each tablet ranges from 1 to 200 mg . Secondly , Lee teaches (pg.14, 1 st paragraph under section 2.4) that granules range in size from 0. 8 5 mm to 4.75 mm . Thirdly , the Examiner estimates that a typical tablet would be close in size to Size 1 Capsule , which has a volume of 0.48 mL, a length of 19.4 mm and a diameter of 6.91 mm ( as evidenced by Wikipedia article on “Capsule (pharmacy)” obtained from the website: https://en.wikipedia.org/wiki/Capsule_(pharmacy) – see the table on pg.3 ). As calculated by the Examiner, assuming that granules are spherical, a 0.85 mm granule would have a volume of 0.0003216 mL, and 4.75 mm granule would have a volume of 0.0561 mL. This means that for a tablet that is the size of Size 1 Capsule, there is about 1492 granule s ( 0.48 mL divided by 0.0003216 mL = 1492 ) of size 0.85 mm in a tablet; and there is about 9 granules ( 0.48 mL divided by 0.0561 mL = 8.55 ) of size 4.75 mm in a tablet. Since a tablet can contain from 1 to 200 mg of mitapivat equivalent, this means that the mitapivat equivalent for each granule ranges from 1/1492 mg to 200/9 mg, which is 6.7 x 10 -4 mg to 22.2 mg of mitapivat equivalent for each granule . Such range overlaps with instant range of claim 15, thus rendering instant range prima facie obvious. In re Wertheim, supra . Thus, S izemore in view of CDC chart, Agresta and Lee renders obvious instant claim 15. With respect to instant claims 22-25, the Examiner established above that there is 6.7 x 10 -4 mg to 22.2 mg of mitapivat equivalent for each granule . Instant range “about 1 mg” of mitapivat equivalent for each granule would have been obvious to one skilled in the art before the effective filing date of the claimed invention since it has been held that where the general conditions of a claim are disclosed in the prior art, discovering the optimum or workable ranges involves only routine skill in the art. In re Aller , supra . Alternatively , the range 6.7 x 10 -4 mg to 22.2 mg for the mitapivat equivalent for each granule overlaps with instant range about 1 mg , thus rendering instant range prima facie obvious. In re Wertheim, supra . As to instant limitation as to the amount of mitapivat administered to the pediatric subject being about 20 mg, about 10 mg, or about 2 mg , as discussed above, Sizemore teaches that Crystalline Form A ( instant m itapivat hemisulfate sesquihydrate ) is formulated for administration at a dose equivalent of about 2 mg to about 3000 mg of Compound 1 (instant mitapivat ) . Instant ranges about 20 mg, about 10 mg or about 2mg would have been obvious to one skilled in the art before the effective filing date of the claimed invention since it has been held that where the general conditions of a claim are disclosed in the prior art, discovering the optimum or workable ranges involves only routine skill in the art. In re Aller , supra . Alternatively , Sizemore’s range about 2 mg to about 3000 mg overlaps with instant ranges about 20 mg, about 10 mg or about 2mg , thus rendering instant ranges prima facie obvious. In re Wertheim, supra . Instant limitations as to the age range (about 2 hears of age o less than about 12 years of age) and the body weight range (about 20 kg to less than about 40 kg) were already addressed above. Thus, S izemore in view of CDC chart, Agresta and Lee renders obvious instant claim s 22-25 . With respect to instant claim s 56 -57 , the Examiner established above that it would have been obvious to one skilled in the art to use Sizemore’s Crystalline Form A in granular form and sprinkle it on food before administering to a human child . Such granules teach instant minitablet of claim 56. With respect to instant limitation as to each minitablet comprising about 0.1 mg to about 5 mg of mitapivat equivalent , the Examiner already established above that there is 6.7 x 10 -4 mg to 22.2 mg of mitapivat equivalent for each granule . Instant range about 0.1 mg to about 5 mg would have been obvious to one skilled in the art before the effective filing date of the claimed invention since it has been held that where the general conditions of a claim are disclosed in the prior art, discovering the optimum or workable ranges involves only routine skill in the art. In re Aller , supra . Alternatively , the range 6.7 x 10 -4 mg to 22.2 mg for the mitapivat equivalent for each granule overlaps with instant range about 0.1 mg to about 5 mg, thus rendering instant range prima facie obvious. In re Wertheim, supra . As to instant range for the longest dimension or diameter being a length of about 10.0 mm to about 0.1 mm , as already discussed above, Lee teaches (pg.14, 1 st paragraph under section 2.4) that granules range in size from 0.85 mm to 4.75 mm . Such range falls within instant range of about 0.1 mm to about 10.0mm , and thus teaches instant range. The limitation “ wherein the minitablet is suitable for mixing with food before oral administration once or twice daily to patients with difficulties swallowing ” was already addressed above. Also, the subject matter of claim 57 was already discussed above in relation to instant claim 1. Thus, S izemore in view of CDC chart, Agresta and Lee renders obvious instant claims 56 and 57, With respect to instant claim 58 , as already discussed above, Lee (see both paragraphs under Introduction on pg.1 ; pg.2, left-hand column, 1 st paragraph) teaches even though dosage forms like capsules and tablets are preferred due to dosing convenience, high physicochemical stability and cost-effectiveness, the large size of sold formulations is challenging for patients with dysphagia ( often the elderly and children ) to swallow, which in turn promoted the development of sprinkle formulations. Lee teaches that Sprinkle formulations are drug containing pellets or granules that can be mixed with soft food before administration. The food taken together with the drug can also mask the unpleasant taste and smell of the drug substance which potentially improves patient compliance. Since Sizemore teaches ([0219]) that its Crystalline Form A ( instant mitapivat hemisulfate sesquihydrate ) can be formed into a tablet either through dry or wet granulation (Sizemore also teaches ([0053]) that the subject in need of treatment can be a human adult over 18 years old) , it would have been obvious to one skilled in the art to use Sizemore’s Crystalline Form A in granular form (instead of tablet form) and sprinkle it on food before administering to the elderly having dysphagia with a reasonable expectation of making Crystalline Form A easier to swallow for the elderly and maksing any unpleasant taste and smell of Crystalline Form A so as to improve patience compliance. Thus, S izemore in view of CDC chart, Agresta and Lee renders obvious instant claim 58. Any inquiry concerning this communication or earlier communications from the examiner should be directed to SIN J. LEE whose telephone number is (571)272-1333. The examiner can normally be reached on M-F 9 am-5:30pm. If attempts to reach the examiner by telephone are unsuccessful, the examiner’s supervisor, Brian Kwon can be reached on 571-272-0581. The fax phone number for the organization where this application or proceeding is assigned is 571-273-8300. Information regarding the status of an application may be obtained from the Patent Application Information Retrieval (PAIR) system. Status information for published applications may be obtained from either Private PAIR or Public PAIR. Status information for unpublished applications is available through Private PAIR only. For more information about the PAIR system, see http://pair-direct.uspto.gov. Should you have questions on access to the Private PAIR system, contact the Electronic Business Center (EBC) at 866-217-9197 (toll-free). Examiner interviews are available via telephone, in-person, and video conferencing using a USPTO supplied web-based collaboration tool. To schedule an interview, Applicant is encouraged to use the USPTO Automated Interview Request (AIR) at http://www.uspto.gov/interviewpractice . /SIN J LEE/ Primary Examiner, Art Unit 1613 December 13, 202 5
Read full office action

Prosecution Timeline

Mar 23, 2023
Application Filed
Jul 07, 2025
Response after Non-Final Action
Dec 13, 2025
Non-Final Rejection — §103 (current)

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Study what changed to get past this examiner. Based on 5 most recent grants.

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Prosecution Projections

1-2
Expected OA Rounds
69%
Grant Probability
94%
With Interview (+25.5%)
3y 0m
Median Time to Grant
Low
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