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IMPORTANT SAFETY INFORMATION & INDICATION

IMPORTANT SAFETY INFORMATION

CONTRAINDICATIONS

TARPEYO is contraindicated in patients with hypersensitivity to budesonide or any of the ingredients of TARPEYO. Serious hypersensitivity reactions, including anaphylaxis, have occurred with other budesonide formulations.

WARNINGS AND PRECAUTIONS

Hypercorticism and adrenal axis suppression:

When corticosteroids are used chronically, systemic effects such as hypercorticism and adrenal suppression may occur. Corticosteroids can reduce the response of the hypothalamus-pituitary-adrenal (HPA) axis to stress. In situations where patients are subject to surgery or other stress situations, supplementation with a systemic corticosteroid is recommended. When discontinuing therapy or switching between corticosteroids, monitor for signs of adrenal axis suppression.

Patients with moderate to severe hepatic impairment (Child-Pugh Class B and C, respectively) could be at an increased risk of hypercorticism and adrenal axis suppression due to an increased systemic exposure to oral budesonide. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C). Monitor for increased signs and/or symptoms of hypercorticism in patients with moderate hepatic impairment (Child-Pugh Class B).

Immunosuppression and increased risk of infection:

Corticosteroids, including TARPEYO, suppress the immune system and increase the risk of infection with any pathogen, including viral, bacterial, fungal, protozoan, or helminthic pathogens. Corticosteroids can: reduce resistance to new infections, exacerbate existing infections, increase the risk of disseminated infections, increase the risk of reactivation or exacerbation of latent infections, and mask some signs of infection. Corticosteroid-associated infections can sometimes be serious. Monitor for infection and consider TARPEYO withdrawal as needed.

Avoid corticosteroid therapy, including TARPEYO, in patients with active or quiescent tuberculosis or hepatitis B infection; untreated fungal, bacterial, systemic viral, or parasitic infections; ocular herpes simplex; or Kaposi’s sarcoma. Avoid exposure to active, easily transmitted infections (e.g., chickenpox, measles). Corticosteroid therapy may decrease the immune response to some vaccines.

Other corticosteroid effects:

TARPEYO is a systemically available corticosteroid and is expected to cause related adverse reactions. Monitor patients with hypertension, prediabetes, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, or with a family history of diabetes or glaucoma, or with any other condition where corticosteroids may have unwanted effects.

ADVERSE REACTIONS

In clinical studies, the most common adverse reactions with TARPEYO (occurring in ≥5% of TARPEYO-treated patients, and ≥2% higher than placebo) were peripheral edema (17%), hypertension (12%), muscle spasms (12%), acne (11%), headache (10%), upper respiratory tract infection (8%), face edema (8%), weight increased (7%), dyspepsia (7%), dermatitis (6%), arthralgia (6%), and white blood cell count increased (6%).

DRUG INTERACTIONS

Budesonide is a substrate for CYP3A4. Avoid use with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine. Avoid ingestion of grapefruit juice with TARPEYO. Intake of grapefruit juice, which inhibits CYP3A4 activity, can increase the systemic exposure to budesonide.

USE IN SPECIFIC POPULATIONS

Pregnancy:

The available data from published case series, epidemiological studies, and reviews with oral budesonide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with IgAN. Infants exposed to in utero corticosteroids, including budesonide, are at risk for hypoadrenalism.

INDICATION

TARPEYO is indicated to reduce the loss of kidney function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression.

Please see Full Prescribing Information.

mod

Elevated systemic Gd-IgA1 can lead to immune complex formation and mesangial deposition1

The gut-kidney axis plays a significant role in the pathophysiology of IgAN2

  • Gd-IgA1 is an emerging biomarker and is widely considered to be an initial step in IgAN pathogenesis3,4
  • Peyer's patches are thought to be a predominant source of Gd-IgA1 in IgAN2

NEARLY

Graphic stating that nearly 50% of Peyer’s patch tissue is located in the human distal ileum, highlighted in large neon-style text.

of Peyer’s patch tissue has been shown to be found in the distal ileum5,6

IgAN is a progressive immune-mediated disease where early modulation is important2,3

The widely accepted 4-HIT model illustrates the pathogenesis of IgAN3:

Diagram of the 4-HIT model explaining IgAN pathogenesis: Gd-IgA1 enters circulation, forms autoantibodies, creates immune complexes, and deposits in kidneys. Diagram of the 4-HIT model explaining IgAN pathogenesis: Gd-IgA1 enters circulation, forms autoantibodies, creates immune complexes, and deposits in kidneys.

In the phase 3 NefIgArd trial, levels of circulating Gd-IgA were reduced from baseline at 3, 6, and 9 months with TARPEYO + RASi vs RASi alone. Data are exploratory. Clinical significance has not been established. Small sample sizes of a specific patient group are limitations of these analyses.

*Mucosal B cells present in the ileum, including the Peyer’s patches, express glucocorticoid receptors, and are responsible for the production of Gd-IgA1 causing IgAN. Through their anti-inflammatory and immunosuppressive effects at the glucocorticoid receptor, corticosteroids can modulate B cell numbers and activity. It has not been established to what extent the efficacy of TARPEYO is mediated via local effects in the ileum vs systemic effects.7,9
†TARPEYO was studied under the name Nefecon, which was used in the 2025 KDIGO guideline.

product design

TARPEYO is designed to locally target a key site of Gd-IgA1 production10*

Budesonide is a locally acting glucocorticoid designed to limit the systemic exposure due to a high rate of first-pass liver metabolism10

A graphic illustrating the proprietary TARPEYO technology and its components: On the left, it shows the immunomodulating active ingredient, Budesonide, with its molecular structure depicted. In the center, it highlights the triple-coated beads designed to help control the rate of release. On the right, it shows the enteric coat for delayed release, with an illustration of a capsule containing these beads (4 mg per capsule). A graphic illustrating the proprietary TARPEYO technology and its components: On the left, it shows the immunomodulating active ingredient, Budesonide, with its molecular structure depicted. In the center, it highlights the triple-coated beads designed to help control the rate of release. On the right, it shows the enteric coat for delayed release, with an illustration of a capsule containing these beads (4 mg per capsule).

It has not been established to what extent the efficacy of TARPEYO is mediated via local effects in the ileum vs systemic effects.

*Mucosal B cells present in the ileum, including the Peyer’s patches, express glucocorticoid receptors, and are responsible for the production of Gd-IgA1 causing IgAN. Through their anti-inflammatory and immunosuppressive effects at the glucocorticoid receptor, corticosteroids can modulate B cell numbers and activity.7,9

TARPEYO is designed to target the distal ileum, including the Peyer’s patches, to treat IgAN at a key site* of Gd-IgA1 production7,11

Local action and first-pass metabolism

  • Budesonide is a locally acting glucocorticoid designed to limit systemic exposure due to high rate of first-pass liver metabolism10

Shorter half-life and exposure duration

  • In pharmacokinetic studies comparing TARPEYO and Entocort® EC (budesonide), TARPEYO exhibited higher maximum plasma concentrations of budesonide while having a shorter terminal half-life, indicating a shorter duration of systemic exposure to budesonide13

Clinical significance is unknown.

Prolonged retention

  • Developed for topical use on mucosal surfaces, budesonide exhibits rapid absorption and prolonged retention in mucosal tissue10

It has not been established to what extent the efficacy of TARPEYO is mediated via local effects in the ileum vs systemic effects.

WATCH OUR MOA VIDEO TO LEARN MORE
A video thumbnail titled 'MOA Video,' providing a concise, informative video on TAPPEYO’s mechanism of action.

In the phase 3 NefIgArd trial, levels of circulating Gd-IgA1 were reduced from baseline at 3, 6, and 9 months with TARPEYO + RASi vs RASi alone. Data are exploratory. Clinical significance has not been established. Small sample sizes of a specific patient group are limitations of these analyses.

*Mucosal B cells present in the ileum, including the Peyer’s patches, express glucocorticoid receptors, and are responsible for the production of Gd-IgA1 causing IgAN. Through their anti-inflammatory and immunosuppressive effects at the glucocorticoid receptor, corticosteroids can modulate B cell numbers and activity.7,9

TARPEYO is the only formulation of budesonide designed to target the Peyer’s patches of the ileum10,14

An in vitro study compared the release patterns of commercially available oral budesonide products. Its aim was to determine if the products are interchangeable regarding their delivery of budesonide to the GI tract.14*

Findings suggest that the release pattern of TARPEYO is consistent with the intended design of the product, to deliver budesonide to the Peyer’s patch-rich area of the ileum.15

Dissolution profiles of 3 delayed-release budesonide oral formulations14,15

Graph showing dissolution rates of TARPEYO, Entocort, and Uceris over 180 minutes. TARPEYO shows delayed release, reaching ~80% at 180 minutes, compared to faster release in Entocort and Uceris. Graph showing dissolution rates of TARPEYO, Entocort, and Uceris over 180 minutes. TARPEYO shows delayed release, reaching ~80% at 180 minutes, compared to faster release in Entocort and Uceris.

Approximate GI tract transit time (highly variable; illustrative only and not intended to compare efficacy and safety). TARPEYO was studied under the name Nefecon.

  • TARPEYO demonstrated a unique dissolution profile compared to other budesonide formulations, including Entocort EC14
  • The release pattern of TARPEYO indicates that the delivery of budesonide would occur in the ileum14

*Dissolution test conditions were conducted based on EMA, FDA, and USP guidelines.14

gd-iga1

POST HOC SUBANALYSIS: Reductions in Gd-IgA1 were seen with TARPEYO10,16*†

In a post hoc biomarker subanalysis of NefIgArd, serum Gd-IgA1 was reduced at months 3, 6, and 910,16

Percent (%) change in Gd-IgA1 with TARPEYO + RASi vs RASi alone10

Line graph showing percent change from baseline over 12 months. Patients on TARPEYO + RASi experienced a decrease during treatment (-11.8% at Month 9) with partial rebound at Month 12 (+8.9%), while RASi alone group showed steady increase, reaching +25% by Month 12. Line graph showing percent change from baseline over 12 months. Patients on TARPEYO + RASi experienced a decrease during treatment (-11.8% at Month 9) with partial rebound at Month 12 (+8.9%), while RASi alone group showed steady increase, reaching +25% by Month 12.

Data are exploratory. Clinical significance has not been established. Small sample sizes of a specific patient group are limitations of these analyses. Additional longitudinal studies of more diverse patient cohorts are needed to validate findings.

  • Reductions in IgG anti-IgA autoantibodies and IgA-containing immune complexes were also seen with TARPEYO16

*Data from Part A of the Phase 3 NeflgArd trial.
†Mucosal B cells present in the ileum, including the Peyer’s patches, express glucocorticoid receptors, and are responsible for the production of Gd-IgA1 causing IgAN. Through their anti-inflammatory and immunosuppressive effects at the glucocorticoid receptor, corticosteroids can modulate B cell numbers and activity. It has not been established to what extent the efficacy of TARPEYO is mediated via local effects in the ileum vs systemic effects.7,9
‡TARPEYO was studied under the name Nefecon, which was used in the KDIGO 2025 guideline.

VIEW DOSING

EMA=European Medicines Agency; FDA=Food and Drug Administration; GALT=gut-associated lymphoid tissue; Gd-IgA1=galactose-deficient IgA1; GI=gastrointestinal; IgA=immunoglobulin A; IgG=immunoglobulin G; KDIGO=Kidney Disease: Improving Global Outcomes; RASi=renin-angiotensin system inhibitor; USP=United States Pharmacopeia.

REFERENCES: 1. Lim RS, Yeo SC, Barratt J, et al. An update on current therapeutic options in IgA nephropathy. J Clin Med. 2024;13(4):947. doi:10.3390/jcm13040947 2. Barratt J, Rovin BH, Cattran D, et al. Why target the gut to treat IgA nephropathy? Kidney Int Rep. 2020;5(10):1620-1624. doi:10.1016/j.ekir.2020.08.009 3. Chang S, Li X-K. The role of immune modulation in pathogenesis of IgA nephropathy. Front Med (Lausanne). 2020;7:92. doi:10.3389/fmed.2020.00092 4. Kim JS, Hwang HS, Sang HL, et al. Clinical relevance of serum galactose deficient IgA1 in patients with IgA nephropathy. J Clin Med. 2020;9:3549. 5. Jung C, Hugot J-P, Barreau F. Peyerʼs patches: the immune sensors of the intestine. Int Journal Inflammation. 2010;1-12. https://doi.org/10.4061/2010/823710 6. Van Kruiningen H, West AB, Freda BJ, et al. Distribution of Peyerʼs patches in the distal ileum. Inflammatory Bowel Dis. 2002;8(3):180-185. https://doi.org/10.1097/00054725-200205000-00004 7. TARPEYO. Prescribing Information. Calliditas Therapeutics AB; June 2024. 8. Kidney Disease: Improving Global Outcomes (KDIGO). KDIGO 2025 clinical practice guideline for the management of immunoglobulin A nephropathy (IgAN) and immunoglobulin A vasculitis (IgAV). Kidney Int. 2025;108:S1-S71. 9. Lafayette R, Kristensen J, Stone A, et al. Efficacy and safety of a targeted-release formulation of budesonide in patients with primary IgA nephropathy (NefIgArd): 2-year results from a randomized phase 3 trial. Lancet. 2023. http://doi.org/10.1016/S0140-6736(23)01554-4 10. Data on file. Calliditas Therapeutics AB. 11. Barratt J, Kristensen J, Stone A, et al. Nefecon treatment provides kidney benefits for patients with IgAN that extend to those with low levels of UPCR: a sub-analysis of the phase III NefIgArd trial. Kid Int Rep. 2024;9:S1-S662. 12. U.S. Department of Health and Human Services, et al. FDA Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. 45th Edition. 2025. Accessed October 30, 2025. https://www.fda.gov/media/71474/download?attachment 13. Barratt J, Kristensen J, Pedersen C, Jerling M. Insights on Nefecon®, a targeted-release formulation of budesonide and its selective immunomodulatory effects in patients with IgA nephropathy. Drug Des Devel Ther. 2024;18:3415-3428. doi:10.2147/DDDT.S383138 14. Dressman, J. Comparative dissolution of budesonide from four commercially available products for oral administration: implications for interchangeablity. Dissolution Technol. 2023;30(4):224-229. 15. Dressman J, Philipson R, Barratt J. Comparison of the dissolution profile of Nefecon with three other commercially available oral formulations of budesonide: Implications for interchangeability. Poster presented at: IIgANN Congress; September 28-30, 2023; Tokyo, Japan. 16. Khan I, Nawaz N, Jama AAA, et al. Effects of nefecon on Hits 1, 2, and 3 of the IgAN pathogenic cascade: a full NefIgArd analysis. Leicester IgAN research group: Poster presented at 62nd ERA Congress. June 4-7, 2025; Vienna, Austria.

IMPORTANT SAFETY INFORMATION

CONTRAINDICATIONS

TARPEYO is contraindicated in patients with hypersensitivity to budesonide or any of the ingredients of TARPEYO. Serious hypersensitivity reactions, including anaphylaxis, have occurred with other budesonide formulations.

WARNINGS AND PRECAUTIONS

Hypercorticism and adrenal axis suppression:

When corticosteroids are used chronically, systemic effects such as hypercorticism and adrenal suppression may occur. Corticosteroids can reduce the response of the hypothalamus-pituitary-adrenal (HPA) axis to stress. In situations where patients are subject to surgery or other stress situations, supplementation with a systemic corticosteroid is recommended. When discontinuing therapy or switching between corticosteroids, monitor for signs of adrenal axis suppression.

Patients with moderate to severe hepatic impairment (Child-Pugh Class B and C, respectively) could be at an increased risk of hypercorticism and adrenal axis suppression due to an increased systemic exposure to oral budesonide. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C). Monitor for increased signs and/or symptoms of hypercorticism in patients with moderate hepatic impairment (Child-Pugh Class B).

Immunosuppression and increased risk of infection:

Corticosteroids, including TARPEYO, suppress the immune system and increase the risk of infection with any pathogen, including viral, bacterial, fungal, protozoan, or helminthic pathogens. Corticosteroids can: reduce resistance to new infections, exacerbate existing infections, increase the risk of disseminated infections, increase the risk of reactivation or exacerbation of latent infections, and mask some signs of infection. Corticosteroid-associated infections can sometimes be serious. Monitor for infection and consider TARPEYO withdrawal as needed.

Avoid corticosteroid therapy, including TARPEYO, in patients with active or quiescent tuberculosis or hepatitis B infection; untreated fungal, bacterial, systemic viral, or parasitic infections; ocular herpes simplex; or Kaposi’s sarcoma. Avoid exposure to active, easily transmitted infections (e.g., chickenpox, measles). Corticosteroid therapy may decrease the immune response to some vaccines.

Other corticosteroid effects:

TARPEYO is a systemically available corticosteroid and is expected to cause related adverse reactions. Monitor patients with hypertension, prediabetes, diabetes mellitus, osteoporosis, peptic ulcer, glaucoma or cataracts, or with a family history of diabetes or glaucoma, or with any other condition where corticosteroids may have unwanted effects.

ADVERSE REACTIONS

In clinical studies, the most common adverse reactions with TARPEYO (occurring in ≥5% of TARPEYO-treated patients, and ≥2% higher than placebo) were peripheral edema (17%), hypertension (12%), muscle spasms (12%), acne (11%), headache (10%), upper respiratory tract infection (8%), face edema (8%), weight increased (7%), dyspepsia (7%), dermatitis (6%), arthralgia (6%), and white blood cell count increased (6%).

DRUG INTERACTIONS

Budesonide is a substrate for CYP3A4. Avoid use with potent CYP3A4 inhibitors, such as ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine. Avoid ingestion of grapefruit juice with TARPEYO. Intake of grapefruit juice, which inhibits CYP3A4 activity, can increase the systemic exposure to budesonide.

USE IN SPECIFIC POPULATIONS

Pregnancy:

The available data from published case series, epidemiological studies, and reviews with oral budesonide use in pregnant women have not identified a drug-associated risk of major birth defects, miscarriage, or other adverse maternal or fetal outcomes. There are risks to the mother and fetus associated with IgAN. Infants exposed to in utero corticosteroids, including budesonide, are at risk for hypoadrenalism.

INDICATION

TARPEYO is indicated to reduce the loss of kidney function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression.

Please see Full Prescribing Information.

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