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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 Gd-IgA1 IS ASSOCIATED WITH IMMUNE COMPLEX FORMATION AND MESANGIAL DEPOSITION1

  • The gut-kidney axis plays a significant role in the pathophysiology of IgA nephropathy2
  • Peyer’s patches are lymphoid follicles within the GALT that are in greatest concentration in the distal ileum where the majority of Gd-IgA1 is thought to be produced2
  • Gd-IgA1 is an emerging biomarker that has been correlated with CKD progression3

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 ileum4,5

IgA NEPHROPATHY (IgAN) IS A PROGRESSIVE IMMUNE-MEDIATED DISEASE WHERE EARLY MODULATION IS IMPORTANT2,6

The widely accepted 4-HIT model illustrates the pathogenesis of IgAN6:

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.
product design

TARPEYO IS A TARGETED-RELEASE CAPSULE DESIGNED TO DELIVER BUDESONIDE TO A KEY SITE OF Gd-IgA1 PRODUCTION10

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).

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, TARPEYO exhibited higher maximum plasma concentrations of budesonide while having a shorter terminal half-life, indicating a shorter duration of systemic exposure to budesonide11

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.

TARPEYO IS THE ONLY FORMULATION OF BUDESONIDE DESIGNED TO TARGET THE PEYER’S PATCHES OF THE ILEUM10,12

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.12*

Findings suggest that the release pattern of TARPEYO is consistent with the intended design of the product, to deliver budesonide to the Peyerʼs patch-rich area of the ileum.12

Dissolution profiles of 3 delayed-release budesonide oral formulations12,13

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 Entocort12
  • The release pattern of TARPEYO indicates that the delivery of budesonide would occur in the ileum12

*Dissolution test conditions were conducted based on EMA, FDA, and USP guidelines.12

DISCOVER DOSING

EMA=European Medicines Agency; FDA=Food and Drug Administration; GALT=gut-associated lymphoid tissue; Gd-IgA1=galactose-deficient IgA1; GI=gastrointestinal; IgA1=immunoglobulin A1; IgG=immunoglobulin G; 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. 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. 4. 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 5. 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 6. 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 7. Zeng Q, Wang WR, Li YH, et al. Diagnostic and prognostic value of galactose-deficient IgA1 in patients with IgA nephropathy: an updated systematic review with meta-analysis. Front Immunol. 2023;14:1209394. doi:10.3389/fimmu.2023.1209394 8. Canetta PA, Kiryluk K, Appel GB. Glomerular diseases: emerging tests and therapies for IgA nephropathy. Clin J Am Soc Nephrol. 2014;9(3):617-625. 9. Kidney Disease: Improving Global Outcomes (KDIGO). KDIGO 2024 clinical practice guideline for the management of immunoglobulin A nephropathy (IgAN) and immunoglobulin A vasculitis (IgAV). Public Review Draft; August 2024. Accessed June 10, 2025. https://kdigo.org/wp-content/uploads/2024/08/KDIGO-2024-IgAN-IgAV-Guideline-Public-Review-Draft.pdf 10. Data on file. Calliditas Therapeutics AB. 11. 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 12. Dressman J. Comparative dissolution of budesonide from four commercially available products for oral administration: implications for interchangeablity. Dissolution Technol. 2023;30(4):224-229. 13. 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. 14. U.S. Department of Health and Human Services, et al. FDA Orange Book: Approved Drug Products with Therapeutic Equivalence Evaluations. 44th Edition. 2024. Accessed June 10, 2025. https://www.fda.gov/media/71474/download?attachment

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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This site is intended only for US residents. The products discussed in this site may have different product labeling in different countries.

TARPEYO is a registered trademark of Calliditas Therapeutics AB, or its affiliates.

© Calliditas Therapeutics AB
All rights reserved.  06/25 US-TAR-2400170 v4.0

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