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mesalamine 375 mg Capsule, Extended Release, 120-count — NDC 68682-113-20 (Billing 68682-0113-20)

by Oceanside Pharmaceuticals · 1 BOTTLE in 1 CARTON / 120 CAPSULE, EXTENDED RELEASE in 1 BOTTLE

This is a package of 120 capsules of mesalamine 375 mg Capsule, Extended Release from Oceanside Pharmaceuticals, no longer marketed (first marketed Jul 2018), no longer in the FDA NDC Directory; retail pharmacies pay about $0.7274 per capsule (NADAC). It is this product's only package size.

NDC 68682-0113-20
🏷️ FDA NDC (as labeled) 68682-113-20 billing pads the product segment with a zero
Rx only Brand Discontinued Non-controlled ⚠ Discontinued by firm ⇄ Compare with another NDC
🗂️ FDA directory synced Oct 8, 2026 · this listing last changed Jul 24, 2026 · sources: openFDA · FDA label (DailyMed) · FDA Orange & Purple Book · First Databank · CMS NADAC, ASP, Medicare & Medicaid · RxNorm
📋 All sources & update times →

This page is curated, coded, and maintained by

Compiled from public FDA, CMS, DailyMed, NADAC, and related drug data sources. Editorial policy

NDC database record

One package, one record: these facts belong to NDC 68682-113-20 alone.

Record
FDA NDC Directory package listing · Human prescription drug
Code segments
68682 labeler · 113 product · 20 package
Package marketed since
Jul 19, 2018
Sample package
No — commercial package
Listing certified through
Dec 31, 2026
Billing quantity
120 EA per package
Barcode (UPC)
0368682113204
FDA record last changed
Jul 24, 2026
⚠️
Other active recalls for Mesalamine (different manufacturers) — 1 · tap to view
These affect other manufacturers’ products for the same ingredient — not necessarily the exact NDC on this page.
Class II · Feb 5, 2024 — Failed Dissolution Specifications: Out of specification for dissolution. (SUN PHARMACEUTICAL INDUSTRIES INC) · FDA recall D-0350-2024
Each entry is an official FDA enforcement report — look up any recall number in the FDA recall database ↗
⚠️
Excluded from the active FDA NDC Directory. The labeler reported this product as discontinued, so it is excluded from the active NDC Directory. The listing was last certified through Apr 2026. A label may still appear on DailyMed, but the NDC is no longer in the current FDA NDC Directory. Search the FDA NDC Directory ↗

Identity & classification

Regulatory identifiers FDA, NLM and CMS codes for this package

FDA NDC (as labeled) 68682-113-20
Product NDC 68682-113
11-digit billing NDC 68682011320
NCPDP billing unit EA — each (per item)
RxCUI 825130
UNII 4Q81I59GXC
UPC 0368682113204
Application # NDA022301
SPL Set ID cfe4800f-868f-46fd-8b9a-977a91ae5fbe
Established class (EPC) Aminosalicylate
Chemical class Aminosalicylic Acids
DEA schedule Non-controlled
Marketing category NDA AUTHORIZED GENERIC
Marketing status Discontinued
FDA listing status Discontinued by firm (certified through Apr 2026)
Marketing start 2018-07-19
Route ORAL
Dosage form CAPSULE, EXTENDED RELEASE
Substance MESALAMINE
TE code (Orange Book) AB · RLD · RS

Drug-database identifiers Medi-Span GPI and First Databank GCN / HICL / AHFS classification

GPI-14 52500030007020
GPI class Mesalamine ER
GCN Seq No 064701
GCN 16159
HICL code 001848
Ingredient (HICL) Mesalamine
HIC1 code D
Therapeutic class — broad (HIC1) Biliary System/Gastro-Intestinal System
HIC2 code D6
Therapeutic class — intermediate (HIC2) Drugs Acting Principally On The Colon
HIC3 code D6F
Therapeutic class — specific (HIC3) Drug Tx-Chronic Inflam. Colon Dx,5-Aminosalicylat
AHFS code 56:36.00.00
AHFS class Anti-Inflammatory Agents (Gi Drugs)
FDB label name MESALAMINE ER 0.375 GRAM CAP
FDB brand name Mesalamine Er
Legend status F — Federal legend — prescription drug or device
Quick answers
  • GSN (GCN sequence number): 064701
  • GCN: 16159
  • GPI-14 (Medi-Span): 52500030007020
  • HICL (First Databank): 001848
  • AHFS class code: 56:36.00.00
  • RxCUI (RxNorm): 825130
Why two NDCs? The FDA registers this code as 68682-113-20 — a 5-3-2 layout, and that's what's printed on the package and shown on DailyMed. For insurance claims, every NDC is standardized to a uniform 11-digit 5-4-2 format by adding a zero to the product segment → 68682-0113-20. Same drug, same package — only the format differs.
Where does this data come from?
Identifiers from the FDA openFDA NDC Directory and Structured Product Labeling; RxCUI from RxNorm (NLM); GPI from Medi-Span; GCN / HIC / AHFS / legend from First Databank.

RxNorm drug class

This medicine belongs to the Aminosalicylate class.

Pharmacologic class Aminosalicylate
Drug family (ATC) Aminosalicylic acid and similar agents
Where does this data come from?
Therapeutic classes from RxNorm RxClass (U.S. National Library of Medicine) — Established Pharmacologic Class (FDA), ATC drug family (WHO) and mechanism of action, matched by this product’s RxCUI.

Clinical

Label name MESALAMINE ER 0.375 GRAM CAP Ingredient Mesalamine
📖 What it is MedlinePlus · NLM

Mesalamine is used to treat ulcerative colitis (a condition which causes swelling and sores in the lining of the colon [large intestine] and rectum) and also to maintain improvement of ulcerative colitis symptoms. Mesalamine is in a class of medications called anti-inflammatory agents. It works by stopping the body from producing a certain substance that may cause inflammation.

Read the full MedlinePlus article ↗
📗 Our plain-language guide HelloPharmacist
  • It treats ulcerative colitis and, in rectal forms, inflammation in the lower bowel such as proctitis. Some products are for flares, some for keeping remission, and some for both. Y...
  • It depends on your product. Tablets and most capsules are swallowed whole. Rectal forms are usually used at bedtime. Drink plenty of fluids, and follow your label for food and timi...
  • Headache, gas, belly pain and diarrhea are the common ones. Call your doctor if you get severe cramping with bloody diarrhea, fever or rash, since that could be a reaction to the d...
  • Yes. Your kidney function should be checked before starting and periodically after. If you take azathioprine or 6-mercaptopurine, or are 65 or older, blood counts should be monitor...
📖 Read our full Mesalamine guide →
Where does this data come from?
Plain-language summary from MedlinePlus (U.S. National Library of Medicine); supplement & herbal interactions and nutrient depletion data from the Natural Medicines database; our full guide is HelloPharmacist editorial content.

Pricing

A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.

Price systemPer eaPer package
Retail pharmacies payNADAC · weekly $0.727 $87.29 / 120 capsules
Medicaid paysCMS SDUD · 12 mo No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data.
Medicare drug plans payPart D · Q2 2026 $1.16 $139.36 / 120 capsules
NADAC price history (per ea) — tap or hover for the price & month
Dec 2021 Apr 2022 Sep 2022 Feb 2024 $1.927 $0.727
▼ Down 62% over the last 15 months.
Where does this data come from?
NADAC (National Average Drug Acquisition Cost) is the CMS weekly pharmacy-acquisition-cost survey — what pharmacies pay. ASP (Average Sales Price) is the CMS Medicare Part B drug-payment file, published quarterly. Medicaid pays is computed by us from CMS State Drug Utilization Data (total reimbursed ÷ units, trailing 12 months) — gross of rebates and inclusive of dispensing fees, so it reflects what Medicaid paid, not an acquisition cost. Medicare drug plans pay is the median negotiated point-of-sale unit cost across plans listing this NDC in the CMS quarterly Prescription Drug Plan pricing files, before rebates. The VA pays is the federal contract price (FSS, and the statutory Big 4 ceiling where listed) from the VA National Acquisition Center pharmaceutical price file. All are free public government data; each measures a different payer, so the figures are not directly comparable.

Packaging — all sizes for this product

Package NDCDescription Marketing startMarketing endStatus
68682-0113-20 You're viewing this Main listing 1 BOTTLE in 1 CARTON / 120 CAPSULE, EXTENDED RELEASE in 1 BOTTLE 2018-07-19 — Discontinued by firm

Therapeutic equivalents

ProductLabelerPackNADAC/unitTEStatusPrice vs. this
mesalamine 375 mg 00093-9224-89 Teva 120 capsules $0.478 AB Availability likely save 34%
Mesalamine .375 g 00378-1375-78 Mylan 120 capsules $0.478 AB Availability likely save 34%
Mesalamine .375 g 00832-6056-12 Upsher-Smith 120 capsules $0.478 AB Availability likely save 34%
Mesalamine .375 g 50268-0577-15 AvPAK 1 capsule $0.478 AB Availability likely save 34%
Mesalamine .375 g 59651-0397-08 Aurobindo 120 capsules $0.478 AB Availability likely save 34%
Mesalamine .375 g 60687-0650-32 American 1 capsule $0.478 AB Availability likely save 34%
Mesalamine .375 g 62332-0724-35 Alembic 120 capsules $0.478 AB Availability likely save 34%
Mesalamine .375 g 68382-0452-19 Zydus 120 capsules $0.478 AB Availability likely save 34%
mesalamine 375 mgthis 68682-0113-20 Oceanside 120 capsules $0.727 AB Discontinued —
Mesalamine 375 mg 31722-0489-12 Camber 120 capsules — AB FDA listed —
Mesalamine .375 g 46708-0724-35 Alembic 120 capsules — AB FDA listed —
Mesalamine .375 g 50742-0371-12 Ingenus 120 capsules — AB FDA listed —
Mesalamine .375 g 51407-0976-12 Golden 120 capsules — AB FDA listed —
Apriso 375 mg 65649-0103-01 Salix 4 capsules — AB FDA listed —
Mesalamine .375 g 67877-0717-05 Ascend 500 capsules — AB FDA listed —
Mesalamine .375 g 70771-1625-07 Zydus 120 capsules — AB FDA listed —
About this product: this is an authorized generic — the brand-name product marketed without its brand name. Other versions are listed above, least expensive first.
Where does this data come from?
Equivalents are other NDCs of the same ingredient, form and route from the openFDA NDC Directory, ranked least-expensive-first by NADAC. Therapeutic-equivalence (AB) ratings come from the FDA Orange Book; biologics use the FDA Purple Book for biosimilar & interchangeable status.

Availability & generic status

🏛️
2008
First FDA approval
Oct 2008
📍
2026
Currently FDA-listed
18 years listed
🛡️
2030
Latest patent/protection listed
not a guaranteed launch date
✅Generic appears available

FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.

🛡️ Latest patent/protection date listed: FDA patent/protection data lists protections through May 2030. This may affect when a full generic version becomes widely available, but it is not a guaranteed launch date.
📅 FDA approved Oct 31, 2008 AB TE-rated RLD RS ⏳ ~3.6 yr to latest listed protection

Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.

Patents & exclusivity — FDA Orange Book
US 8865688 — method of use (U-1310)
2008 2010 2012 2014 2016 2018 2020 2022 2024 2026 2028 2030
Today
LOE
Substance patent Formulation patent Method-of-use patent Exclusivity Pediatric +6mo
🏛️FDA exclusivity
FDA-granted marketing protection. It’s separate from patents and may be shorter than patent protection.
🧪Product / substance patents
Patents covering the active ingredient, product, formulation, or related drug features.
🎯Method-of-use patents
Patents covering specific approved uses. These can sometimes be carved out with a “skinny label,” but not always.
🛈 What do these terms mean?
Patent
Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
Substance patent
Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
Formulation (product) patent
Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
Method-of-use patent
A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
Skinny label
A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
Exclusivity
FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
Paragraph IV
A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
RLD / RS
Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
TE / AB rating
FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
LOE (loss of exclusivity)
The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.

Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.

Listed patents (1)
PatentTypeUse codeExpires
US 8865688 ↗ Method of use U-1310 May 1, 2030
Common questions
Is there a generic version of MESALAMINE ER 0.375 GRAM CAP?
Yes — an FDA-approved generic equivalent is listed in the FDA Orange Book for MESALAMINE ER 0.375 GRAM CAP. See the alternatives section for substitutable, lower-cost products.
The FDA approved a generic — why can’t I get it at my pharmacy yet?
FDA approval and pharmacy availability are two different things. The FDA can approve a generic years before it actually reaches pharmacies, because the brand company may still hold patents or have a settlement that delays the launch. A manufacturer also has to choose to make and sell it, and have supply ready. So a drug can be “FDA-approved generic exists” and still be brand-only at the counter today.
Why do different websites show different generic release dates?
Generic availability is not based on one single date. Some sources use the first exclusivity expiration, some use the last product patent, and others use the latest method-of-use patent. Patent challenges, settlements, licenses, and label carve-outs can also change the real-world launch date. This page shows the underlying Orange Book dates so you can see why estimates may differ.
What does “FDA listed” mean?
It means the product appears in the FDA’s official NDC directory. That’s a good sign a product exists and is intended for the U.S. market, but on its own it does not confirm a pharmacy can fill it today. Where we have recent retail pricing data (NADAC) for a product, we label it “Availability likely” instead.
What does a patent or protection date mean here?
It’s the latest date currently listed in the FDA Orange Book for a patent or exclusivity on the brand product. It can affect when a full generic version becomes widely available — but it is not a guaranteed generic launch date. Generics sometimes arrive earlier (through a settlement or patent challenge) or later (a manufacturer still has to make and sell one).
What does “current Orange Book estimate” mean?
It means we are using the latest patent and exclusivity dates currently listed in the FDA Orange Book. It is not a guaranteed launch date.
Can a generic come out before the last patent expires?
Sometimes. A generic company may challenge a patent, settle with the brand manufacturer, receive a license, or obtain approval with a narrower label that avoids a patented use. In other cases, the last listed protection may delay full-label generic competition.
Can a generic come out after the listed dates?
Yes. Even after patents or exclusivity expire, a generic still needs FDA approval and a manufacturer must choose to market it. Supply, litigation, business decisions, or regulatory issues can delay actual availability.
What is the difference between patents and exclusivity?
Patents are legal protections usually issued by the U.S. Patent and Trademark Office. FDA exclusivity is marketing protection granted by the FDA. They are separate, and either one can affect generic timing.
Why are there multiple patent dates?
One drug can have several patents covering different things: the active ingredient, a formulation, a manufacturing process, or a specific approved use. That is why a page may show several expiration dates instead of one simple generic date.
Built from FDA Orange Book patent and exclusivity data. Dates are refreshed from public FDA data when available; the marker is max(latest patent expiry, latest exclusivity expiry). Paragraph-IV settlements and first-filer 180-day exclusivity can shift the real date; a method-of-use patent may allow an earlier skinny-label generic for non-protected indications. Generic launch timing is an estimate, not a guarantee.
Where does this data come from?
Patents and exclusivity from the FDA Orange Book (small-molecule drugs), refreshed from public FDA data. Generic launch timing is an estimate, not a guarantee.

Inactive Ingredients / Excipients

Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.

🧪 Avoiding an ingredient? See Mesalamine inactive ingredients by manufacturer: every current product's list side by side, so you can ask your pharmacy for the version that does not list it.

We could not link this NDC to a current FDA Structured Product Label. An inactive-ingredient list is therefore not available from this source.
Where does this data come from?
Source: official FDA Structured Product Labeling (SPL) via DailyMed and the openFDA label index. Structured IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.

Inactive ingredient FAQ

Are inactive ingredients the same for every manufacturer?
No. Inactive ingredients can differ by manufacturer, dosage form, strength, and package / product version.
Why might an inactive ingredient be missing?
Some SPLs do not provide a complete structured inactive-ingredient list, and older or unusual labels may only include the information in narrative text.
Can inactive ingredients matter?
Yes. They can matter for allergies, intolerances, dyes, gluten / lactose concerns, preservatives, and formulation differences — but confirm with a pharmacist or the manufacturer when it’s clinically important.

Manufacturer & labeler

LabelerOceanside Pharmaceuticals
Application holderSALIX PHARMACEUTICALS INC
FDA applicationNDA022301 (NDA AUTHORIZED GENERIC)
Labeler code68682
First marketedJul 2018
Product typeHuman Prescription Drug
Portfolio87 products on file

More NDCs from Oceanside Pharmaceuticals labeler code 68682

The labeler markets the product; the application holder owns the FDA approval. They’re often the same company but can differ (e.g. a repackager or an authorized generic). A mailing address / phone appears here when the manufacturer includes it in the product’s FDA label (not all do).
Where does this data come from?
Labeler, application holder and registered establishment from the FDA openFDA NDC Directory and Drugs@FDA; address/contact from the product’s FDA label.

Full prescribing information FDA SPL

The complete FDA label for this product — the official prescribing information, verbatim, section by section. Very long sections are excerpted here and marked; the full text is on DailyMed (linked in the sources below). Jump with a chip, search within the label, or expand everything.
🎯 Indications and Usage ⏱️ Dosage and Administration 💊 Dosage Forms and Strengths ⛔ Contraindications ⚠️ Warnings and Cautions 🤒 Adverse Reactions 🔄 Drug Interactions 👥 Use in Specific Populations 🤰 Pregnancy 🧒 Pediatric Use 🧓 Geriatric Use 🆘 Overdosage 🧬 Clinical Pharmacology 🧬 Mechanism of Action 📦 How Supplied / Storage and Handling 📋 Description 💬 Information for Patients 🧬 Pharmacokinetics 🔬 Clinical Studies 🧪 Nonclinical Toxicology 📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 📄 Package Label / Principal Display Panel
🎯 Indications and Usage 37 words ▾

1 INDICATIONS AND USAGE Mesalamine extended-release capsules are indicated for the maintenance of remission of ulcerative colitis in adults. Mesalamine is an aminosalicylate indicated for the maintenance of remission of ulcerative colitis in adults. ( 1 )

⏱️ Dosage and Administration 182 words ▾

2 DOSAGE AND ADMINISTRATION Dosage The recommended dosage in adults is 1.5 g (four 0.375 g capsules) orally once daily in the morning. Administration Instructions Evaluate renal function before initiating therapy with mesalamine extended-release capsules [ see Warnings and Precautions (5.1) ] . Swallow mesalamine extended-release capsules whole.

Do not cut, break, crush or chew the capsules. Avoid co-administration of mesalamine extended-release capsules with antacids [ see Drug Interactions (7.1 ) ]. Drink an adequate amount of fluids [ see Warnings and Precautions (5.7) ].

Take mesalamine extended-release capsules without regard to meals [ see Clinical Pharmacology (12.3 ) ] . Dosage The recommended dosage is 1.5 g (four 0.375 g capsules) once daily in the morning. ( 2 ) Administration Instructions Evaluate renal function before initiating therapy with mesalamine extended-release capsules.

( 2 ) Swallow the capsules whole. Do not cut, break, crush or chew the capsules. ( 2 ) Avoid co-administration with antacids.

( 2 , 7.1 ) Drink an adequate amount of fluids. ( 2 , 5.7 ) Take mesalamine extended-release capsules without regard to meals. ( 2 )

💊 Dosage Forms and Strengths 38 words ▾

3 DOSAGE FORMS AND STRENGTHS Extended-release capsules: 0.375 g mesalamine in a light blue opaque gelatin capsule with the letters “G” and “M” imprinted on either side of a black band. Extended-release capsules: 0.375 g ( 3 )

⛔ Contraindications 57 words ▾

4 CONTRAINDICATIONS Mesalamine extended-release capsules are contraindicated in patients with hypersensitivity to salicylates or aminosalicylates or to any of the components of mesalamine extended-release capsules [ see Warnings and Precautions (5.3), Adverse Reactions (6.2), Description (11) ] . Known or suspected hypersensitivity to salicylates, aminosalicylates, or any component of mesalamine extended-release capsules. ( 4 , 5.3 )

⚠️ Warnings and Cautions ~2 min read ▾

5 WARNINGS AND PRECAUTIONS Renal Impairment: Assess renal function at the beginning of treatment and periodically during treatment. Evaluate the risks and benefits in patients with known renal impairment or taking nephrotoxic drugs; monitor renal function. Discontinue if renal function deteriorates.

( 5.1 , 7.2 , 8.6 ) Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may be difficult to distinguish from an exacerbation of ulcerative colitis; monitor for worsening symptoms; discontinue treatment if acute intolerance syndrome is suspected. ( 5.2 ) Hypersensitivity Reactions, including Myocarditis and Pericarditis: Evaluate patients immediately and discontinue if a hypersensitivity reaction is suspected. ( 5.3 ) Hepatic Failure: Evaluate the risks and benefits in patients with known liver impairment.

( 5.4 ) Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation. ( 5.5 ) Photosensitivity : Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors. ( 5.6 ) Nephrolithiasis: Mesalamine-containing stones are undetectable by standard radiography or computed tomography (CT).

Ensure adequate fluid intake during treatment. ( 5.7 ) Risks in Patients with Phenylketonuria : Contains phenylalanine. Before prescribing mesalamine extended-release capsules to a patient with PKU, consider the combined daily amount of phenylalanine from all sources, including mesalamine extended-release capsules.

( 5.8 ) Interference with Laboratory Tests : Use of mesalamine may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection. ( 5.9 )

5.1Renal Impairment Renal impairment, including minimal change disease, acute and chronic interstitial nephritis, and renal failure, has been reported in patients given products such as mesalamine extended-release capsules that contain mesalamine or are converted to mesalamine. In animal studies, the kidney was the principal organ of mesalamine toxicity [ see Adverse Reactions (6.2) , Nonclinical Toxicology (13.2) ]. Evaluate renal function prior to initiation of mesalamine extended-release capsules therapy and periodically while on therapy.

Evaluate the risks and benefits of using mesalamine extended-release capsules in patients with known renal impairment or a history of renal disease or taking concomitant nephrotoxic drugs. Discontinue mesalamine extended-release capsules if renal function deteriorates while on therapy [see Drug Interactions (7.2) , Use in Specific Populations (8.6) ].

5.2Mesalamine-Induced Acute Intolerance Syndrome Mesalamine has been associated with an acute intolerance syndrome that may be difficult to distinguish from an exacerbation of ulcerative colitis. Although the exact frequency of occurrence has not been determined, it has occurred in 3% of patients in controlled clinical trials of mesalamine or sulfasalazine. Symptoms include cramping, acute abdominal pain and bloody diarrhea, sometimes fever, headache, and rash.

Monitor patients for worsening of these symptoms while on treatment. If acute intolerance syndrome is suspected, promptly discontinue treatment with mesalamine extended-release capsules.

5.3Hypersensitivity Reactions Some patients have experienced a hypersensitivity reaction to sulfasalazine. Some patients may have a similar reaction to mesalamine extended-release capsules or to other compounds that contain or are converted to mesalamine. As with sulfasalazine, mesalamine-induced hypersensitivity reactions may present as internal organ involvement, including myocarditis, pericarditis, nephritis, hepatitis, pneumonitis and hematologic abnormalities.

Evaluate patients immediately if signs or symptoms of a hypersensitivity reaction are present. Discontinue mesalamine extended-releas… [Excerpted — this section continues on DailyMed.]

🤒 Adverse Reactions ~3 min read ▾

6 ADVERSE REACTIONS The following clinically significant adverse reactions are described elsewhere in labeling: Renal Impairment [ see Warnings and Precautions (5.1) ] Mesalamine-Induced Acute Intolerance Syndrome [ see Warnings and Precautions (5.2) ] Hypersensitivity Reactions [ see Warnings and Precautions (5.3) ] Hepatic Failure [ see Warnings and Precautions (5.4) ] Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.5 )] Photosensitivity [ see Warnings and Precautions (5.6) ] Nephrolithiasis [ see Warnings and Precautions (5.7) ] Risks in Patients with Phenylketonuria [ see Warnings and Precautions (5.8) ] Most common adverse reactions (≥3%) are: headache, diarrhea, upper abdominal pain, nausea, and nasopharyngitis.

( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Oceanside Pharmaceuticals at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

6.1Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The data described below reflect exposure to mesalamine extended-release capsules in 557 patients, including 354 exposed for at least 6 months and 250 exposed for greater than one year. Mesalamine extended-release capsules were studied in two placebo-controlled trials (n=367 treated with mesalamine extended-release capsules) and in one open-label, long-term study (n=190 additional patients).

The population consisted of patients with ulcerative colitis; the mean age was 47 years, 54% were female, and 93% were white. Patients received doses of mesalamine extended-release capsules 1.5 g administered orally once per day for six months in the placebo-controlled trials and for up to 24 months in the open‑label study. In the two placebo-controlled trials, the most common reactions reported in at least 3% of mesalamine extended-release capsules-treated patients and at a greater rate than placebo are shown in Table 1 below.

Table 1: Common Adverse Reactions Reported in at least 3% of mesalamine extended-release capsules-treated patients and at a greater rate than with placebo in Clinical Trials of Adults with Ulcerative Colitis Mesalamine Extended-Release Capsules 1.5 g once daily N=367 Placebo N=185 Headache 11% 8% Diarrhea 8% 7% Upper Abdominal Pain 5% 3% Nausea 4% 3% Nasopharyngitis 4% 3% The following adverse reactions, presented by body system, were reported at a frequency less than 3% in patients treated with mesalamine extended-release capsules for up to 24 months in controlled and open-label trials.

Ear and Labyrinth Disorders : tinnitus, vertigo Dermatological Disorder : alopecia Gastrointestinal : lower abdominal pain, rectal hemorrhage Laboratory Abnormalities : increased triglycerides, decreased hematocrit and hemoglobin General Disorders and Administration Site Disorders : fatigue Hepatic : hepatitis cholestatic, transaminases increased Renal Disorders : creatinine clearance decreased, hematuria Musculoskeletal : pain, arthralgia Respiratory : dyspnea

6.2Postmarketing Experience The following adverse reactions have been identified during post approval use of mesalamine extended-release capsules or other mesalamine-containing products. Because many of these reactions are reported voluntarily from a population of unknown size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Body as a Whole : lupus-like syndrome, drug fever Cardiovascular : pericarditis, pericardial effusion, myocarditis [see Warnings and Precautions (5.3 )] Gastrointestinal : pancreatitis, cholecystitis, gastritis, gastroenteritis, gastrointestinal bleeding, perforated peptic ulcer Hepatic : jaundice, cholestatic jaundice, hepatitis, liver necrosis, liver failure, Kawasaki-like syndrome including changes in liver enzymes… [Excerpted — this section continues on DailyMed.]

🔄 Drug Interactions ~1 min read ▾

7 DRUG INTERACTIONS Nephrotoxic Agents including NSAIDs: Increased risk of nephrotoxicity; monitor for changes in renal function and mesalamine-related adverse reactions. ( 7.2 ) Azathioprine or 6-Mercaptopurine: Increased risk of blood disorders; monitor complete blood cell counts and platelet counts. ( 7.3 )

7.1Antacids Because the dissolution of the coating of the granules in mesalamine extended-release capsules depends on pH, avoid co-administration of mesalamine extended-release capsules with antacids [ see Dosage and Administration (2) ] .

7.2Nephrotoxic Agents, Including Non-Steroidal Anti-Inflammatory Drugs The concurrent use of mesalamine with known nephrotoxic agents, including non-steroidal anti-inflammatory drugs (NSAIDs) may increase the risk of nephrotoxicity. Monitor patients taking nephrotoxic drugs for changes in renal function and mesalamine-related adverse reactions [ see Warnings and Precautions (5.1) ].

7.3Azathioprine or 6-Mercaptopurine The concurrent use of mesalamine with azathioprine or 6-mercaptopurine and/or other drugs known to cause myelotoxicity may increase the risk for blood disorders, bone marrow failure, and associated complications. If concomitant use of mesalamine extended-release capsules and azathioprine or 6-mercaptopurine cannot be avoided, monitor blood tests, including complete blood cell counts and platelet counts.

7.4Interference with Urinary Normetanephrine Measurements Use of mesalamine extended-release capsules may lead to spuriously elevated test results when measuring urinary normetanephrine by liquid chromatography with electrochemical detection [ see Warnings and Precautions (5.9) ] . Consider an alternative, selective assay for normetanephrine.

👥 Use in Specific Populations ~3 min read ▾

8 USE IN SPECIFIC POPULATIONS Geriatric Patients : Increased risk of blood dyscrasias; monitor blood cell counts and platelet counts. ( 8.5 )

8.1Pregnancy Risk Summary Published data from meta-analyses, cohort studies and case series on the use of mesalamine during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data) . In animal reproduction studies, there were no adverse developmental outcomes with administration of oral mesalamine during organogenesis to pregnant rats and rabbits at doses 1.7 and 5.4 times, respectively, the maximum recommended human dose (see Data) .

The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Clinical Considerations Disease-associated maternal and embryo/fetal risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with ulcerative colitis. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. Data Human Data Published data from meta-analyses, cohort studies and case series on the use of mesalamine during early pregnancy (first trimester) and throughout pregnancy have not reliably informed an association of mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes.

There is no clear evidence that mesalamine exposure in early pregnancy is associated with an increased risk in major congenital malformations, including cardiac malformations. Published epidemiologic studies have important methodological limitations which hinder interpretation of the data, including inability to control for confounders, such as underlying maternal disease, and maternal use of concomitant medications, and missing information on the dose and duration of use for mesalamine products. Animal Data Reproduction studies with mesalamine during organogenesis have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human dose based on a body surface area comparison) and rabbits at doses up to 495 mg/kg/day (about 5.4 times the recommended human dose based on a body surface area comparison) and have revealed no evidence of harm to the fetus due to mesalamine.

8.2Lactation Risk Summary Data from published literature report the presence of mesalamine and its metabolite, N-acetyl 5-aminosalicylic acid in human milk in small amounts with relative infant doses (RID) of 2% or less (see Data) . There are case reports of diarrhea in breastfed infants exposed to mesalamine (see Clinical Considerations) . There is no information on the effects of the drug on milk production.

The lack of clinical data during lactation precludes a clear determination of the risk of mesalamine extended-release capsules to an infant during lactation; therefore, the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for mesalamine extended-release capsules and any potential adverse effects on the breastfed child from mesalamine extended-release capsules or from the underlying maternal condition. Clinical Considerations Advise the caregiver to monitor the breastfed infant for diarrhea.

Data In published lactation studies, maternal mesalamine doses from various oral and rectal formulations and products ranged from 500 mg to 4.8 g daily. The average concentration of mesalamine in milk ranged from non-detectable to 0.5 mg/L. The average concentration of the N-acetyl-5-aminosalicylic acid in milk ranged from 0.2 to 9.3… [Excerpted — this section continues on DailyMed.]

🤰 Pregnancy ~2 min read ▾

8.1Pregnancy Risk Summary Published data from meta-analyses, cohort studies and case series on the use of mesalamine during pregnancy have not reliably informed an association with mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes (see Data) . In animal reproduction studies, there were no adverse developmental outcomes with administration of oral mesalamine during organogenesis to pregnant rats and rabbits at doses 1.7 and 5.4 times, respectively, the maximum recommended human dose (see Data) .

The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. Adverse outcomes in pregnancy occur regardless of the health of the mother or the use of medications. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.

Clinical Considerations Disease-associated maternal and embryo/fetal risk Published data suggest that increased disease activity is associated with the risk of developing adverse pregnancy outcomes in women with ulcerative colitis. Adverse pregnancy outcomes include preterm delivery (before 37 weeks of gestation), low birth weight (less than 2500 g) infants, and small for gestational age at birth. Data Human Data Published data from meta-analyses, cohort studies and case series on the use of mesalamine during early pregnancy (first trimester) and throughout pregnancy have not reliably informed an association of mesalamine and major birth defects, miscarriage, or adverse maternal or fetal outcomes.

There is no clear evidence that mesalamine exposure in early pregnancy is associated with an increased risk in major congenital malformations, including cardiac malformations. Published epidemiologic studies have important methodological limitations which hinder interpretation of the data, including inability to control for confounders, such as underlying maternal disease, and maternal use of concomitant medications, and missing information on the dose and duration of use for mesalamine products. Animal Data Reproduction studies with mesalamine during organogenesis have been performed in rats at oral doses up to 320 mg/kg/day (about 1.7 times the recommended human dose based on a body surface area comparison) and rabbits at doses up to 495 mg/kg/day (about 5.4 times the recommended human dose based on a body surface area comparison) and have revealed no evidence of harm to the fetus due to mesalamine.

🧒 Pediatric Use 17 words ▾

8.4Pediatric Use Safety and effectiveness of mesalamine extended-release capsules in pediatric patients have not been established.

🧓 Geriatric Use 126 words ▾

8.5Geriatric Use Clinical studies of mesalamine extended-release capsules did not include sufficient numbers of subjects aged 65 years and older to determine whether they respond differently than younger subjects. Reports from uncontrolled clinical studies and postmarketing reporting systems suggested a higher incidence of blood dyscrasias (i.e., agranulocytosis, neutropenia and pancytopenia) in patients who were 65 years or older compared to younger patients taking mesalamine-containing products such as mesalamine extended-release capsules.

Monitor complete blood cell counts and platelet counts in elderly patients during treatment with mesalamine extended-release capsules. In general, consider the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy in elderly patients when prescribing mesalamine extended-release capsules [ see Use in Specific Populations (8.6) ] .

🆘 Overdosage 117 words ▾

10 OVERDOSAGE Mesalamine is an aminosalicylate, and symptoms of salicylate toxicity include nausea, vomiting and abdominal pain, tachypnea, hyperpnea, tinnitus, and neurologic symptoms (headache, dizziness, confusion, seizures). Severe salicylate intoxication may lead to electrolyte and blood pH imbalance and potentially to other organ (e.g., renal and liver) damage. There is no specific antidote for mesalamine overdose; however, conventional therapy for salicylate toxicity may be beneficial in the event of acute overdosage and may include gastrointestinal tract decontamination to prevent further absorption.

Correct fluid and electrolyte imbalance by the administration of appropriate intravenous therapy and maintain adequate renal function. Mesalamine extended-release capsules are a pH-dependent delayed-release product and this factor should be considered when treating a suspected overdose.

🧬 Clinical Pharmacology ~3 min read ▾

12 CLINICAL PHARMACOLOGY

12.1Mechanism of Action The mechanism of action of mesalamine (5-ASA) is not fully understood, but appears to be a local anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites.

12.3Pharmacokinetics Absorption The pharmacokinetics of 5-ASA and its metabolite, N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA), were studied after a single and multiple oral doses of 1.5 g mesalamine extended-release capsules in a crossover study in healthy subjects under fasting conditions. In the multiple-dose period, each subject received mesalamine extended-release capsules 1.5 g (four 0.375 g capsules) once daily for 7 consecutive days. Steady state was reached on Day 6 of once daily dosing based on trough concentrations.

After single and multiple doses of mesalamine extended-release capsules, peak plasma concentrations were observed at about 4 hours post-dose. At steady state, moderate increases (1.5-fold and 1.7-fold) in systemic exposure (AUC 0-24 ) to 5-ASA and N-Ac-5-ASA were observed when compared with a single-dose of mesalamine extended-release capsules. Pharmacokinetic parameters after a single dose of 1.5 g mesalamine extended-release capsules and at steady state in healthy subjects under fasting condition are shown in Table 2.

Table 2: Single Dose and Multiple Dose Mean (±SD) Plasma Pharmacokinetic Parameters of Mesalamine (5-ASA) and N-Ac-5-ASA After 1.5 g Mesalamine Administration in Healthy Subjects Mesalamine (5-ASA) Single Dose (n=24) Multiple Dose c (n=24) a Median (range); b Harmonic mean (pseudo SD); c after 7 days of treatment AUC 0-24 (mcg*h/mL) 11±5 17±6 AUC 0-inf (mcg*h/mL) 14±5 - C max (mcg/mL) 2.1±1.1 2.7±1.1 T max (h) a 4 (2, 16) 4 (2, 8) t ½ (h) b 9±7 10±8 N-Ac-5-ASA AUC 0-24 (mcg*h/mL) 26±6 37±9 AUC 0-inf (mcg*h/mL) 51±23 - C max (mcg/mL) 2.8±0.8 3.4±0.9 T max (h) a 4 (4, 12) 5 (2, 8) t ½ (h) b 12±11 14±10 In a separate study (n=30), it was observed that under fasting conditions about 32%±11% (mean±SD) of the administered dose was systemically absorbed based on the combined cumulative urinary excretion of 5-ASA and N-Ac-5-ASA over 96 hours post-dose.

Food Effects The effect of a high fat meal intake on absorption of mesalamine granules (the same granules contained in mesalamine extended-release capsules) was evaluated in 30 healthy subjects. Subjects received 1.6 g of mesalamine granules in sachet (2 x 0.8 g) following an overnight fast or a high fat meal in a crossover study. Under fed conditions, T max for both 5-ASA and N‑Ac‑5-ASA was prolonged by 4 and 2 hours, respectively.

A high fat meal did not affect C max for 5-ASA, but a 27% increase in the cumulative urinary excretion of 5-ASA was observed with a high fat meal. The overall extent of absorption of N‑Ac-5-ASA was not affected by a high fat meal [ see Dosage and Administration (2) ] . Distribution In an in vitro study, at 2.5 mcg/mL, mesalamine and N-Ac-5-ASA are 43±6% and 78±1% bound, respectively, to plasma proteins.

Protein binding of N-Ac-5-ASA does not appear to be concentration dependent at concentrations ranging from 1 to 10 mcg/mL. Elimination Metabolism The major metabolite of mesalamine is N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA). It is formed by N-acetyltransferase activity in the liver and intestinal mucosa.

Excretion Following single and multiple doses of mesalamine extended-release capsules, the mean half-lives were 9 to 10 hours for 5-ASA, and 12 to 14 hours for N-Ac-5-ASA. Of the approximately 32% of the dose absorbed, about 2% of the dose was excreted unchanged in the urine, compared with about 30% of the dose excreted as N-Ac-5-ASA. Drug Interaction Studies I… [Excerpted — this section continues on DailyMed.]

🧬 Mechanism of Action 72 words ▾

12.1Mechanism of Action The mechanism of action of mesalamine (5-ASA) is not fully understood, but appears to be a local anti-inflammatory effect on colonic epithelial cells. Mucosal production of arachidonic acid metabolites, both through the cyclooxygenase pathways, i.e., prostanoids, and through the lipoxygenase pathways, i.e., leukotrienes and hydroxyeicosatetraenoic acids, is increased in patients with ulcerative colitis, and it is possible that 5-ASA diminishes inflammation by blocking production of arachidonic acid metabolites.

📦 How Supplied / Storage and Handling 76 words ▾

16 HOW SUPPLIED/STORAGE AND HANDLING Mesalamine extended-release capsules are available as light blue opaque hard gelatin capsules containing 0.375 g mesalamine in a light blue opaque gelatin capsule with the letters “G” and “M” imprinted on either side of a black band and are available in bottles of 120 capsules (NDC 68682-113-20). Storage : Store at 20° to 25°C (68° to 77°F); excursions permitted between 15° and 30°C (59° and 86°F) [see USP Controlled Room Temperature].

📋 Description 124 words ▾

11 DESCRIPTION Each mesalamine extended-release capsule is a delayed- and extended-release dosage form for oral administration. Each capsule contains 0.375 g of mesalamine USP (5-aminosalicylic acid, 5-ASA), an aminosalicylate. The structural formula of mesalamine is: Molecular Weight: 153.14 Molecular Formula: C 7 H 7 NO 3 Each mesalamine extended-release capsule contains granules composed of mesalamine in a polymer matrix with an enteric coating that dissolves at pH 6 and above.

The inactive ingredients of mesalamine extended-release capsules are: anhydrous citric acid, aspartame, colloidal silicon dioxide, edible black ink, hypromellose, magnesium stearate, methacrylic acid copolymer, microcrystalline cellulose, povidone, simethicone emulsion, ethyl acrylate/methyl methacrylate copolymer, talc, titanium dioxide, triethyl citrate, vanilla flavor. Each mesalamine extended-release 0.375 g capsule contains 0.56 mg of phenylalanine. Apriso chemical structure

💬 Information for Patients ~3 min read ▾

17 PATIENT COUNSELING INFORMATION Administration Instruct patients: Swallow the capsules whole. Do not cut, break, crush or chew the capsules. Avoid co-administration of mesalamine extended-release capsules with antacids.

Drink an adequate amount of fluids. Mesalamine extended-release capsules can be taken without regard to meals [ see Dosage and Administration (2) ] . Urine may become discolored reddish-brown while taking mesalamine extended-release capsules when it comes in contact with surfaces or water treated with hypochlorite-containing bleach.

If discolored urine is observed, advise patients to observe their urine flow. Report to the healthcare provider only if urine is discolored on leaving the body, before contact with any surface or water (e.g., in the toilet). Renal Impairment Inform patients that mesalamine extended-release capsules may decrease their renal function, especially if they have known renal impairment or are taking nephrotoxic drugs, including NSAIDs, and periodic monitoring of renal function will be performed while they are on therapy.

Advise patients to complete all blood tests ordered by their healthcare provider [ see Warnings and Precautions (5.1) , Drug Interactions (7.2) ] . Mesalamine-Induced Acute Intolerance Syndrome and Other Hypersensitivity Reactions Inform patients of the signs and symptoms of hypersensitivity reactions. Instruct patients to stop taking mesalamine extended-release capsules and report to their healthcare provider if they experience new or worsening symptoms of Acute Intolerance Syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, and rash) or other symptoms suggestive of mesalamine-induced hypersensitivity [ see Warnings and Precautions (5.2 , 5.3) ] .

Hepatic Failure Inform patients with known liver disease of the signs and symptoms of worsening liver function and advise them to report to their healthcare provider if they experience such signs or symptoms [ see Warnings and Precautions (5.4) ] . Severe Cutaneous Adverse Reactions Inform patients of the signs and symptoms of severe cutaneous adverse reactions. Instruct patients to stop taking mesalamine extended-release capsules and report to their healthcare provider at first appearance of a severe cutaneous adverse reaction or other sign of hypersensitivity [ see Warnings and Precautions (5.5 )] .

Photosensitivity Advise patients with pre-existing skin conditions to avoid sun exposure, wear protective clothing, and use a broad-spectrum sunscreen when outdoors [ see Warnings and Precautions (5.6) ] . Nephrolithiasis Instruct patients to drink an adequate amount of fluids during treatment in order to minimize the risk of kidney stone formation and to contact their healthcare provider if they experience signs or symptoms of a kidney stone (e.g., severe side or back pain, blood in the urine) [ see Warnings and Precautions (5.7) ] .

Patients with Phenylketonuria Inform patients with phenylketonuria (PKU) or their caregivers that each mesalamine extended-release capsule contains aspartame equivalent to 0.56 mg of phenylalanine, so that the recommended adult dosing provides an equivalent of 2.24 mg of phenylalanine per day [ see Warnings and Precautions (5.8) ] . Blood Disorders Inform elderly patients and those taking azathioprine or 6-mercaptopurine of the risk for blood disorders and the need for periodic monitoring of complete blood cell counts and platelet counts while on therapy.

Advise patients to complete all blood tests ordered by their healthcare provider [ see Drug Interactions (7.3) , Use in Specific Populations (8.5) ] . Distributed by: Oceanside Pharmaceuticals, a division of Bausch Health US, LLC Bridgewater, NJ 08807 USA Patented. See https://patents.salix.com/ for US patent information. © 2023 Bausch Health Companies Inc. or its affiliates 9652005 20005420

🧬 Pharmacokinetics ~3 min read ▾

12.3Pharmacokinetics Absorption The pharmacokinetics of 5-ASA and its metabolite, N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA), were studied after a single and multiple oral doses of 1.5 g mesalamine extended-release capsules in a crossover study in healthy subjects under fasting conditions. In the multiple-dose period, each subject received mesalamine extended-release capsules 1.5 g (four 0.375 g capsules) once daily for 7 consecutive days. Steady state was reached on Day 6 of once daily dosing based on trough concentrations.

After single and multiple doses of mesalamine extended-release capsules, peak plasma concentrations were observed at about 4 hours post-dose. At steady state, moderate increases (1.5-fold and 1.7-fold) in systemic exposure (AUC 0-24 ) to 5-ASA and N-Ac-5-ASA were observed when compared with a single-dose of mesalamine extended-release capsules. Pharmacokinetic parameters after a single dose of 1.5 g mesalamine extended-release capsules and at steady state in healthy subjects under fasting condition are shown in Table 2.

Table 2: Single Dose and Multiple Dose Mean (±SD) Plasma Pharmacokinetic Parameters of Mesalamine (5-ASA) and N-Ac-5-ASA After 1.5 g Mesalamine Administration in Healthy Subjects Mesalamine (5-ASA) Single Dose (n=24) Multiple Dose c (n=24) a Median (range); b Harmonic mean (pseudo SD); c after 7 days of treatment AUC 0-24 (mcg*h/mL) 11±5 17±6 AUC 0-inf (mcg*h/mL) 14±5 - C max (mcg/mL) 2.1±1.1 2.7±1.1 T max (h) a 4 (2, 16) 4 (2, 8) t ½ (h) b 9±7 10±8 N-Ac-5-ASA AUC 0-24 (mcg*h/mL) 26±6 37±9 AUC 0-inf (mcg*h/mL) 51±23 - C max (mcg/mL) 2.8±0.8 3.4±0.9 T max (h) a 4 (4, 12) 5 (2, 8) t ½ (h) b 12±11 14±10 In a separate study (n=30), it was observed that under fasting conditions about 32%±11% (mean±SD) of the administered dose was systemically absorbed based on the combined cumulative urinary excretion of 5-ASA and N-Ac-5-ASA over 96 hours post-dose.

Food Effects The effect of a high fat meal intake on absorption of mesalamine granules (the same granules contained in mesalamine extended-release capsules) was evaluated in 30 healthy subjects. Subjects received 1.6 g of mesalamine granules in sachet (2 x 0.8 g) following an overnight fast or a high fat meal in a crossover study. Under fed conditions, T max for both 5-ASA and N‑Ac‑5-ASA was prolonged by 4 and 2 hours, respectively.

A high fat meal did not affect C max for 5-ASA, but a 27% increase in the cumulative urinary excretion of 5-ASA was observed with a high fat meal. The overall extent of absorption of N‑Ac-5-ASA was not affected by a high fat meal [ see Dosage and Administration (2) ] . Distribution In an in vitro study, at 2.5 mcg/mL, mesalamine and N-Ac-5-ASA are 43±6% and 78±1% bound, respectively, to plasma proteins.

Protein binding of N-Ac-5-ASA does not appear to be concentration dependent at concentrations ranging from 1 to 10 mcg/mL. Elimination Metabolism The major metabolite of mesalamine is N-acetyl-5-aminosalicylic acid (N-Ac-5-ASA). It is formed by N-acetyltransferase activity in the liver and intestinal mucosa.

Excretion Following single and multiple doses of mesalamine extended-release capsules, the mean half-lives were 9 to 10 hours for 5-ASA, and 12 to 14 hours for N-Ac-5-ASA. Of the approximately 32% of the dose absorbed, about 2% of the dose was excreted unchanged in the urine, compared with about 30% of the dose excreted as N-Ac-5-ASA. Drug Interaction Studies In an in vitro study using human liver microsomes, 5-ASA and its metabolite, N-Ac-5-ASA, were shown not to inhibit the major CYP enzymes evaluated (CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4).

Therefore, mesalamine and its metabolite are not expected to inhibit the metabolism of other drugs that are substrates of CYP1A2, CYP2C9, CYP2C19, CYP2D6, or CYP3A4.

🔬 Clinical Studies ~2 min read ▾

14 CLINICAL STUDIES Two similar, randomized, double-blind, placebo-controlled, multi-center studies were conducted in a total of 562 adult patients in remission from ulcerative colitis. The study populations had a mean age of 46 years (11% age 65 years or older), were 53% female, and were primarily white (92%). Ulcerative colitis disease activity was assessed using a modified Sutherland Disease Activity Index (DAI), which is a sum of four subscores based on stool frequency, rectal bleeding, mucosal appearance on endoscopy, and physician’s rating of disease activity.

Each subscore can range from 0 to 3, for a total possible DAI score of 12. At baseline, approximately 80% of patients had a total DAI score of 0 or 1.0. Patients were randomized 2:1 to receive either mesalamine extended-release capsules 1.5 g or placebo once daily in the morning for six months.

Patients were assessed at baseline, 1 month, 3 months, and 6 months in the clinic, with endoscopy performed at baseline, at end of study, or if clinical symptoms developed. Relapse was defined as a rectal bleeding subscale score of 1 or more and a mucosal appearance subscale score of 2 or more using the DAI. The analysis of the intent-to-treat population was a comparison of the proportions of patients who remained relapse-free at the end of six months of treatment.

For the table below (Table 3) all patients who prematurely withdrew from the study for any reason were counted as relapses. In both studies, the proportion of patients who remained relapse-free at six months was greater for mesalamine extended-release capsules than for placebo. Table 3: Percentage of Ulcerative Colitis Patients Relapse-Free Relapse counted as rectal bleeding score ≥1 and mucosal appearance score ≥2, or premature withdrawal from study.

Through 6 Months in Mesalamine Extended-Release Capsule Maintenance Studies Mesalamine Extended-Release Capsules 1.5 g once daily % (# no relapse/N) Placebo % (# no relapse/N) Difference (95% C.I.) P-value Study 1 68% (143/209) 51% (49/96) 17% (5.5, 29.2) <0.001 Study 2 71% (117/164) 59% (55/93) 12% (0, 24.5) 0.046 Examination of gender subgroups did not identify difference in response to mesalamine extended-release capsules among these subgroups. There were too few elderly and too few African-American patients to adequately assess difference in effects in those populations.

The use of mesalamine extended-release capsules for treating ulcerative colitis beyond six months has not been evaluated in controlled clinical trials.

🧪 Nonclinical Toxicology ~1 min read ▾

13 NONCLINICAL TOXICOLOGY

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Dietary mesalamine was not carcinogenic in rats at doses as high as 480 mg/kg/day, or in mice at 2,000 mg/kg/day. These doses are about 2.6 and 5.4 times the recommended human dose of granulated mesalamine capsules of 1.5 g/day (30 mg/kg if 50 kg body weight assumed or 1,110 mg/m 2 ), respectively, based on body surface area. Mesalamine was negative in the Ames test, the mouse lymphoma cell (L5178Y/TK+/-) forward mutation test, the sister chromatid exchange assay in the Chinese hamster bone marrow test, and the mouse bone marrow micronucleus test.

No effects on fertility or reproductive performance in male and female rats were observed with oral mesalamine doses up to 320 mg/kg (about 1.7 times the recommended human dose based on body surface area).

13.2Animal Toxicology and/or Pharmacology Renal Toxicity Animal studies with mesalamine (13-week and 26-week oral toxicity studies in rats, and 26-week and 52-week oral toxicity studies in dogs) have shown the kidney to be the major target organ of mesalamine toxicity. Single oral doses of 800 mg/kg (about 2.2 times the recommended human dose, on the basis of body surface area) and 1,800 mg/kg (about 9.7 times the recommended human dose, on the basis of body surface area) of mesalamine were lethal to mice and rats, respectively, and resulted in gastrointestinal and renal toxicity.

Oral doses of 40 mg/kg/day (about 0.20 times the human dose, on the basis of body surface area) produced minimal to slight tubular injury, and doses of 160 mg/kg/day (about 0.90 times the human dose, on the basis of body surface area) or higher in rats produced renal lesions including tubular degeneration, tubular mineralization, and papillary necrosis. Oral doses of 60 mg/kg/day (about 1.1 times the human dose, on the basis of body surface area) or higher in dogs also produced renal lesions including tubular atrophy, interstitial cell infiltration, chronic nephritis, and papillary necrosis.

📄 Carcinogenesis, Mutagenesis, Impairment of Fertility 132 words ▾

13.1Carcinogenesis, Mutagenesis, Impairment of Fertility Dietary mesalamine was not carcinogenic in rats at doses as high as 480 mg/kg/day, or in mice at 2,000 mg/kg/day. These doses are about 2.6 and 5.4 times the recommended human dose of granulated mesalamine capsules of 1.5 g/day (30 mg/kg if 50 kg body weight assumed or 1,110 mg/m 2 ), respectively, based on body surface area. Mesalamine was negative in the Ames test, the mouse lymphoma cell (L5178Y/TK+/-) forward mutation test, the sister chromatid exchange assay in the Chinese hamster bone marrow test, and the mouse bone marrow micronucleus test.

No effects on fertility or reproductive performance in male and female rats were observed with oral mesalamine doses up to 320 mg/kg (about 1.7 times the recommended human dose based on body surface area).

📄 Package Label / Principal Display Panel 25 words ▾

PACKAGE/LABEL PRINCIPAL DISPLAY PANEL Mesalamine extended-release capsules 120 Capsules, Bottle Label NDC 68682-113-20 Rx only MESALAMINE EXTENDED-RELEASE CAPSULES 0.375 g 120 Capsules OCEANSIDE PHARMACEUTICALS carton

Source: FDA Structured Product Labeling, mirrored from DailyMed / openFDA. Prefer the government’s original formatting? View this label on DailyMed ↗

Medicare Part D spend CMS · PART D · 2026 (Q1)

Medicare Part D (outpatient prescription) spending for Mesalamine — the program that covers self-administered drugs. 14 manufacturers.
⚠️ Drug-level data: CMS publishes Part D spending by drug, not by NDC — these figures combine every manufacturer, strength and package size sold under the name Mesalamine. That’s a different level of aggregation than the Medicaid card above, which is specific to this exact 11-digit NDC (pack size included), so the two aren’t directly comparable.
Period
Total Part D spend
$39.58M
Claims incl. refills
102.6K
Beneficiaries
69.2K
Spend / beneficiary
$571.72
Spend / claim
$385.73
Trend by period
💵 About the dollar figures: spending is what Part D plans paid before confidential manufacturer rebates, so the program’s real net cost is lower. A blank patient count means fewer than 11 people — CMS hides counts that small to protect privacy. Source: CMS Medicare Quarterly Part D Spending by Drug (data.cms.gov), updated quarterly.

About this NDC listing & data coverage

Finished prescription product No longer marketed (per FDA listing data)
What data is (and isn’t) available for this NDC — tap to expand
NDC identity (package / product / labeler codes) ✓ Available
Labeler ✓ Available
Product & package description ✓ Available
Marketing category & status ✓ Available
Active ingredient / dosage form / route ✓ Available
FDA label (SPL via DailyMed) ✓ Available
Package photos — Not published for this NDC No photo available yet for this listing.
Inactive ingredients (structured) — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available.
NADAC pharmacy acquisition price (CMS) ✓ Available
Orange Book / therapeutic-equivalence data ✓ Available
HCPCS J-code billing crosswalk — Not published for this NDC Most self-administered / retail products have no J-code — that is normal.
Medicaid utilization (CMS SDUD) — Not published for this NDC CMS reports utilization only for NDCs with Medicaid claims above its privacy threshold.
“Not published” reflects what the public FDA / CMS / NLM sources provide for this exact package code — it is a property of the data feeds, not a judgment about the product.

Questions about this listing

What does the discontinued status mean for this NDC?
The labeler reported a marketing end date (or the listing was delisted), so this specific package is no longer actively marketed. Remaining stock may still be dispensed for a time, and the NDC stays valid for historical records and claims — but data feeds (pricing, labeling) typically stop updating for it. Other package sizes or other manufacturers' versions of the same medication may still be marketed — see the equivalents section where available.
Is the NDC printed on the package the same as the 11-digit billing NDC?
Yes, they identify this exact package in different formats. The form printed on the packaging and shown on DailyMed is the one the FDA registered. Insurance claims use a fixed 11-digit 5-4-2 format, so the short segment is padded with a leading zero and the dashes are dropped. The Identity section at the top of this page lists each form of this code.
Who lists this product with the FDA?
Oceanside Pharmaceuticals is the labeler of record for this NDC — the company under whose FDA-assigned code the package is listed. The labeler may be the manufacturer itself or a distributor marketing the product under its own code.
Do I need a prescription for this product?
This NDC is listed with FDA as a prescription product, so it is dispensed under a prescriber's order. Your pharmacist can tell you whether any over-the-counter forms of the same medication exist.
This page identifies an FDA-listed package (the NDC) and reports public regulatory and pricing data about the listing. It is reference information, not a medical recommendation — talk to your pharmacist or prescriber about your own medication.
Where does this data come from?
Listing facts (marketing category, packager status, marketing dates) from the FDA openFDA NDC Directory; label availability from DailyMed; pricing coverage from CMS NADAC; equivalence scope from the FDA Orange Book.
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For educational and professional reference only — not medical advice. Pricing reflects published NADAC and CMS ASP (free public data) and may differ from your acquisition cost; always verify before billing or dispensing.