Linaclotide
Also sold as: Linzess
Linaclotide is an FDA-approved drug, marketed as Linzess capsules under NDA 202811 and taken orally rather than injected. Its approved labeling covers three indications with three different age floors: irritable bowel syndrome with constipation in adults and pediatric patients 7 years of age and older, chronic idiopathic constipation in adults only, and functional constipation in pediatric patients 2 years of age and older. The label carries a boxed warning stating that 'LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration' — a warning that stops exactly where the youngest approved indication begins. The original 2012 label was adults-only and its boxed warning then contraindicated pediatric patients up to 6 years of age and told prescribers to avoid use in patients 6 through 17. Efficacy in adults was established in two randomised, double-blind, placebo-controlled Phase 3 trials, where the label reports combined responder rates of 12% versus 5% on placebo and 13% versus 3%; the pediatric IBS-C indication rests on an analysis with no placebo comparator. Linaclotide appears in none of Categories 1, 2 or 3 of FDA's 503A bulk drug substances list updated 14 May 2026, an absence that reflects its position as the active ingredient of an approved drug rather than any finding about it.
Which molecule this is. A 14-amino acid peptide and a guanylate cyclase-C (GC-C) agonist. Three things about it cut against the defaults of the peptide market. (1) ROUTE — it is an oral capsule, not an injection. LINZESS is supplied as capsules of 72 mcg, 145 mcg and 290 mcg; those strengths identify the product, and this site publishes no dosing. (2) EXPOSURE — the label states 'LINZESS is minimally absorbed with negligible systemic availability following oral administration', and that plasma concentrations of linaclotide and its active metabolite are below the limit of quantitation, so standard pharmacokinetic parameters cannot be calculated for it. A systemic peptide this is not. (3) TARGET — the label describes linaclotide as structurally related to human guanylin and uroguanylin, binding GC-C and acting locally on the luminal surface of the intestinal epithelium. The molecule most people mean when they say 'peptide' is a systemic injectable; this one works in the gut lumen and is largely recovered in stool as its active metabolite.
FDA status
FDA has approved this as a drug. Approval is always for a specific indication and a specific population — check which one, because it is frequently not the use it is marketed for.
FDA-approved under NDA 202811, originally approved 2012-08-30 as a Type 1 New Molecular Entity. Cross-checked against Drugs@FDA on 2026-08-02: NDA 202811, sponsor listed as ABBVIE (openFDA manufacturer field still reads 'Allergan, Inc.'), three LINZESS capsule products, all marketing status Prescription, none discontinued. Drugs@FDA lists twenty submissions under this application, all with status AP, of which five are efficacy supplements (submission numbers 10, 16, 21, 22 and 23); the most recent, supplement 23, was approved 2026-05-21. Approval is always for a specific indication and population — read the approval record below, because the indications here are narrower and stranger than the one-line 'IBS drug' summary suggests.
“LINZESS® (linaclotide) capsules, for oral use … Initial U.S. Approval: 2012 … LINZESS is a guanylate cyclase-C agonist indicated for treatment of: • Irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older. • Chronic idiopathic constipation (CIC) in adults. • Functional constipation (FC) in pediatric patients 2 years of age and older.”Checked against the source on .
Evidence
Efficacy established by adequate, well-controlled trials in humans.
Administration check RUN, not assumed. NCT00948818 was opened and read on 2026-08-02: intervention type DRUG ('Linaclotide 290 micrograms' and 'Matching placebo'), Phase 3, allocation RANDOMIZED, masking QUADRUPLE, enrolment 803 ACTUAL, lead sponsor Forest Laboratories, status COMPLETED with an ACTUAL completion date of August 2010 and results posted. Linaclotide was ADMINISTERED to humans; it was not measured as an endogenous biomarker, which is the trap that reduces MOTS-c and TB-500 from an apparent five human RCTs to an actual zero. The companion pivotal trial NCT00938717 was checked the same way: Phase 3, randomised, quadruple-masked, placebo-controlled, 805 ACTUAL enrolment, lead sponsor Ironwood Pharmaceuticals, COMPLETED September 2010. Both are named in section 14.1 of the current FDA-approved label as Trials 1 and 2, which is the independent corroboration. SCOPE, and it is narrower than the badge. This tier attaches to the approved indications in the approved oral product, and it is strongest for adults. Two limits are visible in the label itself. First, effect sizes are modest: in Trials 1 and 2 the combined responder rates were 12% versus 5% placebo and 13% versus 3% placebo, recorded below with FDA's own confidence intervals. 'Proven in humans' means efficacy was established in adequate and well-controlled trials, not that most patients respond. Second, the paediatric IBS-C indication does NOT rest on a placebo-controlled result — see the finding below on Trial 8, which had no placebo arm and reports a single-arm responder rate.
“A Phase III, Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Trial of Linaclotide Administered Orally … in Patients With Irritable Bowel Syndrome With Constipation”Checked against the source on .
What FDA actually approved
- Application
- NDA 202811 — Linzess
- Approved indication
- LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 2 years of age and older
Verbatim from section 1 of the label approved 2026-05-21. Read the asymmetry, because it is the part a summary destroys: the three indications carry THREE DIFFERENT age floors. IBS-C is approved from 7 years, functional constipation from 2 years, and chronic idiopathic constipation in ADULTS ONLY — there is no paediatric CIC indication at all. The indication history matters as much as the current text, and each step is sourced separately below. The 2012 original approval was adults-only, for IBS-C and CIC. Paediatric functional constipation for ages 6 to 17 was added 2023-06-12. The IBS-C indication was extended to paediatric patients 7 years and older on 2025-11-04. The functional-constipation floor dropped from 6 years to 2 years on 2026-05-21. `discontinued` is false: Drugs@FDA lists all three LINZESS capsule products with marketing status Prescription. That is true of the BRAND only — every approved generic linaclotide product is discontinued, which is recorded as its own finding below.
“LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 2 years of age and older”Checked against the source on .
What FDA found
FDA’s own words. These are the most citable thing on this site, and the least likely to appear anywhere funded by someone selling the compound.
The 2012 original approval label for LINZESS was for adults only, and its boxed warning was headed 'WARNING: PEDIATRIC RISK'. That label contraindicated LINZESS in pediatric patients up to 6 years of age and told prescribers to avoid use in pediatric patients 6 through 17 years of age.
Recorded because the current label cannot show this and the movement is the story. In 2012 FDA's boxed warning told prescribers to AVOID the drug in every paediatric patient and contraindicated it below six years. Fourteen years later the same application is approved from two years of age for functional constipation and from seven for IBS-C, and the boxed warning has been re-scoped to patients under two. Two readings to avoid. This is not FDA relaxing a safety finding — the underlying nonclinical finding (deaths in neonatal mice from dehydration) is still in the current label and still drives the contraindication. It is the age boundary moving as paediatric trials were actually run. And it is not a general precedent: nothing here transfers to any other peptide, because what changed the label was adequate and well-controlled paediatric trials in an approved product, of which the research-chemical market has none.
LINZESS (linaclotide) capsules — original approval label (NDA 202811, s000) — FDA, 31 August 2012“WARNING: PEDIATRIC RISK … LINZESS is contraindicated in pediatric patients up to 6 years of age. Avoid use of LINZESS in pediatric patients 6 through 17 years of age. Linaclotide caused deaths in young juvenile mice … LINZESS is a guanylate cyclase-C agonist indicated in adults for treatment of: • Irritable bowel syndrome with constipation (IBS-C) … • Chronic idiopathic constipation (CIC)”
Checked against the source on .FDA approved LINZESS to treat functional constipation in pediatric patients 6 to 17 years of age on 12 June 2023, stating that it was the first treatment for pediatric functional constipation. The application received priority review.
FDA's own announcement, and the cleanest available statement of first-in-indication status for this drug. FDA describes the supporting evidence precisely: efficacy was established in a 12-week double-blind, placebo-controlled, randomised, multicentre trial (Trial 7, NCT04026113) 'and supported by efficacy data from adequate and well-controlled trials in adults with chronic idiopathic constipation'. Note the structure — a placebo-controlled paediatric trial PLUS extrapolation from adults, not extrapolation alone. The age range in this 2023 announcement (6 to 17) is not the current indication; the floor moved to 2 years on 2026-05-21 and the ceiling was removed. Cite this document for what happened in 2023, not for what the label says today.
FDA approves first treatment for pediatric functional constipation — FDA, 12 June 2023“FDA has approved Linzess (linaclotide) capsules to treat functional constipation in pediatric patients 6 to 17 years of age. Linzess is the first treatment for pediatric functional constipation.”
Checked against the source on .The IBS-C indication was extended into paediatrics by supplement 22, approved 2025-11-04, whose label reads 'Irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older' and, at that revision, 'Functional constipation (FC) in pediatric patients 6 years of age and older'.
The middle step, recorded against its own document because neither the 2023 announcement nor the current label shows it. Verified by fetching supplement 21's label (approved 2023-06-12) and supplement 22's side by side on 2026-08-02: s021 reads 'Irritable bowel syndrome with constipation (IBS-C) in adults' and 'Functional constipation (FC) in pediatric patients 6 to 17 years of age'; s022 adds paediatric IBS-C from 7 years and opens the FC range upward by replacing '6 to 17 years' with '6 years of age and older'. So the hint that this drug is an adult IBS-C product is a description of the 2012 label, not of the current one, and the paediatric IBS-C indication is roughly nine months old.
LINZESS (linaclotide) capsules — approval label (NDA 202811, s022) — FDA, 5 November 2025“LINZESS is a guanylate cyclase-C agonist indicated for treatment of: • Irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older. (1) • Chronic idiopathic constipation (CIC) in adults. (1) • Functional constipation (FC) in pediatric patients 6 years of age and older. (1)”
Checked against the source on .The efficacy analysis supporting the pediatric IBS-C indication had no placebo comparator. In Trial 8 (NCT04026113), 108 patients were randomised to LINZESS or to a higher than recommended dosage of LINZESS, and 53 patients were evaluated for efficacy. The label reports a single-arm combined responder rate of 30% (95% CI 18% to 44%) with no placebo column and no treatment difference. FDA states the indication is supported by evidence from adequate and well-controlled studies in adults and in pediatric patients 7 to 17 years of age.
The most important qualification on this record, and it is invisible unless you open sections 14.2 and 8.4 of the label. The paediatric IBS-C trial was not linaclotide versus placebo — both arms received linaclotide, and the comparison was against a higher than recommended dosage, which the label reports 'did not demonstrate additional treatment benefit'. Table 6 of the label accordingly shows one column. A 30% responder rate with no control arm is not a treatment effect; the label does not present it as one, and the indication rests on extrapolation from the adult placebo-controlled trials. Contrast the paediatric FUNCTIONAL CONSTIPATION trials, which WERE placebo-controlled: Trial 7 (ages 6 to 17, N=328) reported a treatment difference of 1.3 spontaneous bowel movements per week (95% CI 0.7 to 1.8), and Trial 9 (NCT05652205, ages 2 to 5, N=62 on LINZESS and 61 on placebo) reported 0.7 (95% CI 0.03 to 1.31) — an interval whose lower bound is 0.03, which clears zero by almost nothing. Same drug, same label, three very different evidentiary footings.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“A total of 108 patients were randomized to receive treatment with LINZESS … or a higher than recommended dosage of LINZESS. … A total of 53 patients who received LINZESS … were evaluated for efficacy. … The safety and effectiveness of LINZESS for the treatment of IBS-C have been established in pediatric patients 7 years of age and older. Use of LINZESS for this indication is supported by evidence from adequate and well-controlled studies in adults and pediatric patients 7 to 17 years of age.”
Checked against the source on .In the two pivotal placebo-controlled trials in adults with IBS-C, the label reports combined responder rates (abdominal pain and complete spontaneous bowel movement responder, for at least 9 out of 12 weeks) of 12% on LINZESS versus 5% on placebo in Trial 1, a difference of 7% (95% CI 3.2% to 10.9%), and 13% versus 3% in Trial 2, a difference of 10% (95% CI 6.1% to 13.4%).
Recorded verbatim from Tables 3 and 4 because 'FDA-approved' and 'works for most people' are different claims and the second one is not on this label. On the stricter primary endpoint roughly one in eight patients met the combined responder definition, against one in twenty on placebo. On the looser 6-out-of-12-week endpoint the same trials report 34% versus 21% and 34% versus 14%. The separation is real, statistically significant and replicated across two trials — that is what earns the tier — and it is also modest in absolute terms. Both facts are in the same table. Anyone quoting one without the other is quoting half a document.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“In both trials, the proportion of patients who were responders to LINZESS … was statistically significantly higher than with placebo.”
Checked against the source on .Linaclotide appears in none of Categories 1, 2 or 3 of FDA's 503A bulk drug substances list updated 2026-05-14.
Recorded to close a misreading, not to assert a status. Verified by fetching the document with a browser user-agent and text-extracting it on 2026-08-02: zero hits for 'linaclotide' and zero for 'Linzess' across all seven pages. This absence means something entirely different from BPC-157's absence. BPC-157 was nominated and left Category 2 when the nominators withdrew. Linaclotide was never in this system at all — the 503A bulks nomination route exists for substances that are not already components of approved drug products, and linaclotide is the active ingredient of one. The bulks list can establish absence and nothing more; it cannot distinguish 'withdrawn' from 'never nominated' from 'approved drug, never on the nomination track'. This record therefore carries no 503A status badge at all, because inventing one would assert a fact about a proceeding linaclotide was never part of.
Bulk Drug Substances Nominated for Use in Compounding Under Section 503A of the Federal Food, Drug, and Cosmetic Act — FDA, 14 May 2026Checked against the source on .Drugs@FDA lists three abbreviated new drug applications for linaclotide. Two were approved — Mylan's ANDA 209564 on 2021-02-09 and Aurobindo's ANDA 209611 on 2023-02-07 — and every product under both is marked Discontinued. The third, Actavis Labs FL's ANDA 211255, holds a tentative approval dated 2026-05-19 and has no marketing status.
A generic being approved and a generic being available are different facts, and the gap between them is visible in the database. Both approved linaclotide ANDAs show every product Discontinued, and the third application is only TENTATIVELY approved, which in FDA's own scheme means the application meets the approval requirements but cannot be marketed yet. This record makes no claim about WHY — patent and exclusivity positions are not in this dataset, and the site does not guess at them. What is checkable is the state: as of the 2026-07-31 Drugs@FDA extract, the only linaclotide products with a Prescription marketing status are the three brand LINZESS capsules under NDA 202811.
Drugs@FDA — applications containing linaclotide (openFDA drug/drugsfda) — FDA, 31 July 2026Checked against the source on .
Documented safety signals
Boxed warning — risk of serious dehydration in pediatric patients less than 2 years of age. LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration.
FDA's highest-level warning, and it sits on a drug that is simultaneously approved for two-year-olds. Those two facts are not in tension — they meet exactly at the same age boundary. The contraindication floor is 'less than 2 years' and the youngest approved indication is 'pediatric patients 2 years of age and older'. There is no gap and no overlap. The label's expanded section 5.1 gives the mechanism: in neonatal mice, 'linaclotide increased fluid secretion as a consequence of age-dependent elevated GC-C agonism which was associated with increased mortality within the first 24 hours due to dehydration'. FDA adds that a clinical GC-C ontogeny study in 99 children found insufficient data on GC-C intestinal expression to assess the risk in children under two — so the boundary is drawn at the edge of what was measured, not at a demonstrated safe threshold.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE … LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration.”
Checked against the source on .Diarrhea was the most common adverse reaction in the pooled pivotal placebo-controlled IBS-C trials: 20% of LINZESS-treated patients reported diarrhea versus 3% of placebo-treated patients, severe diarrhea was reported in 2% versus less than 1%, and 5% of LINZESS-treated patients discontinued due to diarrhea versus less than 1% on placebo.
Worth stating in the label's own numbers because the adverse reaction here is a stronger signal than the efficacy one. In the same pivotal trials the combined responder difference was 7 to 10 percentage points; the diarrhea difference was 17 percentage points. The label also records that in open-label long-term trials 29% of patients had their dose reduced or suspended because of adverse reactions, the majority diarrhea or other gastrointestinal reactions, and that most reported cases of diarrhea started within the first two weeks.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“In these trials, 20% of LINZESS-treated patients reported diarrhea compared to 3% of placebo-treated patients. Severe diarrhea was reported in 2% of the LINZESS-treated patients versus less than 1% of the placebo-treated patients, and 5% of LINZESS-treated patients discontinued due to diarrhea vs less than 1% of placebo-treated patients.”
Checked against the source on .In post-marketing experience, severe diarrhea associated with dizziness, syncope, hypotension and electrolyte abnormalities (hypokalemia and hyponatremia) requiring hospitalization or intravenous fluid administration has been reported in patients treated with LINZESS.
The consequence chain the trial incidence table does not show. Diarrhea is the labelled adverse reaction; the reported harm is what follows it — volume and electrolyte loss severe enough for admission or intravenous fluids. This is also the same physiological pathway as the boxed warning, scaled to a different population: fluid secretion driven by GC-C agonism, which kills neonatal mice and dehydrates adults. One mechanism, two warnings.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“In post-marketing experience, severe diarrhea associated with dizziness, syncope, hypotension and electrolyte abnormalities (hypokalemia and hyponatremia) requiring hospitalization or intravenous fluid administration have been reported in patients treated with LINZESS.”
Checked against the source on .LINZESS is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction, in addition to the contraindication in patients less than 2 years of age.
Recorded because it is the contraindication that survives from the 2012 label unchanged while the paediatric one moved, and because it is a screening question rather than a monitoring one. It cannot be answered by the patient alone.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“LINZESS is contraindicated in: Patients less than 2 years of age due to the risk of serious dehydration … Patients with known or suspected mechanical gastrointestinal obstruction.”
Checked against the source on .
Questions people actually ask
Every answer cites the document behind it. Where the honest answer is “nobody knows”, that is the answer you will get.
- Is Linzess (linaclotide) FDA-approved?
Yes. Linaclotide is approved by FDA under NDA 202811 and marketed as LINZESS capsules, with an initial U.S. approval in 2012. The current labeling, approved 21 May 2026, states that 'LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 2 years of age and older'. Read the age floors, because they differ by indication and a summary flattens them: chronic idiopathic constipation is an adults-only indication, IBS-C reaches down to 7 years, and functional constipation reaches down to 2 years. Approval attaches to the approved oral capsule product for these uses and does not travel to anything else.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“LINZESS is indicated for the treatment of: • irritable bowel syndrome with constipation (IBS-C) in adults and pediatric patients 7 years of age and older • chronic idiopathic constipation (CIC) in adults • functional constipation (FC) in pediatric patients 2 years of age and older”
Checked against the source on .- Why does Linzess have a boxed warning if it is approved for young children?
Because the boxed warning and the youngest approved indication meet at the same age line rather than overlapping. FDA's boxed warning reads: 'LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration.' The youngest approved indication is functional constipation in pediatric patients 2 years of age and older. So the warning covers everyone below two and the approval starts at two — no gap, no contradiction. The label's fuller explanation is that in neonatal mice linaclotide 'increased fluid secretion as a consequence of age-dependent elevated GC-C agonism which was associated with increased mortality within the first 24 hours due to dehydration', and that a clinical study measuring GC-C expression in 99 children found insufficient data to assess that risk in children under two. The boundary is drawn where the measurement stops, not at a demonstrated safe threshold.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE … LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration.”
Checked against the source on .- When was Linzess approved for children?
In three separate steps, and the current label shows only the endpoint. FDA approved LINZESS for functional constipation in pediatric patients 6 to 17 years of age on 12 June 2023, announcing that 'Linzess is the first treatment for pediatric functional constipation' and that the application received priority review. FDA then approved supplement 22 on 4 November 2025, whose label extended the IBS-C indication to 'adults and pediatric patients 7 years of age and older' while stating functional constipation for 'pediatric patients 6 years of age and older'. Supplement 23, approved 21 May 2026, lowered the functional-constipation floor again, to 'pediatric patients 2 years of age and older'. None of this changed the adults-only chronic idiopathic constipation indication.
FDA approves first treatment for pediatric functional constipation — FDA, 12 June 2023“FDA has approved Linzess (linaclotide) capsules to treat functional constipation in pediatric patients 6 to 17 years of age. Linzess is the first treatment for pediatric functional constipation.”
Checked against the source on .- How well did linaclotide work in the trials FDA approved it on?
It separated from placebo consistently, and by a modest amount. In the two pivotal double-blind, placebo-controlled trials in adults with IBS-C (Trials 1 and 2, NCT00948818 and NCT00938717), the label reports combined responder rates — patients meeting both the abdominal pain and the complete-spontaneous-bowel-movement criteria for at least 9 of the first 12 weeks — of 12% on LINZESS versus 5% on placebo in Trial 1, a difference of 7% (95% CI 3.2% to 10.9%), and 13% versus 3% in Trial 2, a difference of 10% (95% CI 6.1% to 13.4%). FDA's own summary is that 'In both trials, the proportion of patients who were responders to LINZESS … was statistically significantly higher than with placebo.' On a looser responder definition (at least 6 of 12 weeks) the same trials report 34% versus 21% and 34% versus 14%. For comparison, the same label reports diarrhea in 20% of LINZESS-treated patients versus 3% on placebo. Statistically significant and replicated is what an approval requires; it is not the same claim as most patients responding.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“In both trials, the proportion of patients who were responders to LINZESS … was statistically significantly higher than with placebo.”
Checked against the source on .- Is there a generic version of Linzess?
Approved, but not marketed. Drugs@FDA lists three abbreviated new drug applications for linaclotide: Mylan's ANDA 209564, approved 9 February 2021, and Aurobindo Pharma's ANDA 209611, approved 7 February 2023 — every product under both is marked Discontinued — plus Actavis Labs FL's ANDA 211255, which holds a tentative approval dated 19 May 2026 and has no marketing status. As of the 31 July 2026 Drugs@FDA extract, the only linaclotide products carrying a Prescription marketing status are the three brand LINZESS capsules under NDA 202811. This record makes no claim about why the generics are not on the market; patent and exclusivity positions are not in this dataset.
Drugs@FDA — applications containing linaclotide (openFDA drug/drugsfda) — FDA, 31 July 2026Checked against the source on .- Is linaclotide a peptide you inject?
No. Linaclotide is a 14-amino acid peptide, but the approved product is an oral capsule and the drug is not meant to reach the bloodstream at all. FDA's label states that 'LINZESS is minimally absorbed with negligible systemic availability following oral administration' and that plasma concentrations of linaclotide and its active metabolite are below the limit of quantitation, so standard pharmacokinetic parameters such as AUC, Cmax and half-life cannot be calculated for it. The label describes linaclotide as structurally related to human guanylin and uroguanylin, binding guanylate cyclase-C and acting locally on the luminal surface of the intestinal epithelium, then being proteolytically degraded within the intestinal lumen. It is a useful counterexample to two assumptions this category runs on — that a peptide drug must be injected, and that oral peptides do not get approved.
LINZESS (linaclotide) capsules — Highlights of Prescribing Information (NDA 202811, s023) — FDA, 22 May 2026“LINZESS is minimally absorbed with negligible systemic availability following oral administration. Concentrations of linaclotide and its active metabolite in plasma are below the limit of quantitation … Therefore, standard pharmacokinetic parameters such as area under the curve (AUC), maximum concentration (C max ), and half-life (t ½ ) cannot be calculated.”
Checked against the source on .- Can a compounding pharmacy make linaclotide?
This site cannot answer that from the document it would normally use, and says so rather than guessing. Linaclotide appears in none of Categories 1, 2 or 3 of FDA's 503A bulk drug substances list updated 14 May 2026 — verified by fetching and text-extracting that document on 2 August 2026, which returned zero hits for 'linaclotide' and zero for 'Linzess'. But that absence does not mean for linaclotide what it means for BPC-157. The 503A bulks list is the route for substances that are not already components of approved drug products, and linaclotide is the active ingredient of one: LINZESS capsules under NDA 202811. So the list establishes only that linaclotide was never in that nomination process, which is a different fact from whether a pharmacy may compound with it. Anyone who needs the compounding answer should get it from the statute and their state board, not from this list.
Bulk Drug Substances Nominated for Use in Compounding Under Section 503A of the Federal Food, Drug, and Cosmetic Act — FDA, 14 May 2026Checked against the source on .