Tarpeyo

Budesonide · Capsule, Delayed Release · Oral

Uses

1 INDICATIONS AND USAGE 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. TARPEYO is a corticosteroid indicated to reduce the loss of kidney function in adults with primary immunoglobulin A nephropathy (IgAN) who are at risk for disease progression. ( 1 )

Dosage and administration

The recommended duration of therapy is 9 months, with a dosage of 16 mg administered orally once daily [see Clinical Studies ( 14.1 )] . When discontinuing therapy, reduce the dosage to 8 mg once daily for the last 2 weeks of therapy [see Warnings and Precautions ( 5.1 )] . The delayed release capsules should be swallowed whole in the morning, at least 1 hour before a meal. Do not open, crush or chew. If a dose is missed, take the prescribed dose at the next scheduled time. Do not double the next dose. Safety and efficacy of treatment with subsequent courses of TARPEYO have not been established. The recommended dosage is 16 mg administered orally once daily, in the morning at least 1 hour before a meal. ( 2 ) Swallow whole. Do not open, crush or chew. ( 2 ) When discontinuing, reduce dosage to 8 mg once daily for the last two weeks. ( 2 , 5.1 )

Dosage forms and strengths

Delayed release capsule containing 4 mg budesonide. White coated opaque capsules printed with “CAL10 4MG” in black ink. Delayed release capsules: 4 mg ( 3 )

Contraindications

4 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. Hypersensitivity to budesonide or any of the ingredients in TARPEYO. ( 4 )

Warnings and precautions

Hypercorticism and Adrenal Axis Suppression: Follow general warnings concerning corticosteroids, patients with hepatic impairment may be at increased risk. Taper upon discontinuation. ( 2 , 5.1 , 8.6 , 12.3 ) Immunosuppression and Increased Risk of Infection: Avoid use in patients with active or quiescent tuberculosis infection, untreated fungal, bacterial, systemic viral or parasitic infections, or ocular herpes simplex. May affect vaccine efficacy. ( 5.2 ) Other Corticosteroid Effects: Monitor patients with concomitant conditions where corticosteroids may have unwanted effects (e.g., hypertension, diabetes mellitus). ( 5.3 ) 5.1 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 [see Dosing and Administration ( 2 )] 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 of 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) [see Use in Specific Populations ( 8.6 ), Clinical Pharmacology ( 12.3 )] . 5.2 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 Mask some signs of infection Corticosteroid-associated infections can be mild but can be severe and at times fatal. The rate of infectious complications increases with increasing corticosteroid dosages. Monitor for the development of infection and consider TARPEYO withdrawal as needed. Tuberculosis If TARPEYO is used to treat a condition in patients with latent tuberculosis or tuberculin reactivity, reactivation of tuberculosis may occur. In patients with latent tuberculosis or tuberculin reactivity TARPEYO should be discontinued. Varicella Zoster and Measles Viral Infections Varicella and measles can have a serious or even fatal course in non-immune patients taking corticosteroids, including TARPEYO. In corticosteroid-treated patients who have not had these diseases or are non-immune, particular care should be taken to avoid exposure to varicella and measles: If a TARPEYO-treated patient is exposed to varicella, prophylaxis with varicella zoster immune globulin may be indicated. If varicella develops, treatment with antiviral agents may be considered. If a TARPEYO-treated patient is exposed to measles, prophylaxis with immunoglobulin may be indicated. Hepatitis B Virus Reactivation Hepatitis B virus reactivation can occur in patients who are hepatitis B carriers treated with immunosuppressive dosages of corticosteroids, including TARPEYO. Reactivation can also occur infrequently in corticosteroid-treated patients who appear to have resolved hepatitis B infection. Screen patients for hepatitis B infection before initiating immunosuppressive treatment with TARPEYO. For patients who show evidence of hepatitis B infection, recommend consultation with physicians with expertise in managing hepatitis B regarding monitoring and consideration for hepatitis B antiviral therapy. Fungal Infections Corticosteroids, including TARPEYO, may exacerbate systemic fungal infections; therefore, avoid TARPEYO use in the presence of such infections. Amebiasis Corticosteroids, including TARPEYO, may activate latent amebiasis. Therefore, it is recommended that latent amebiasis or active amebiasis be ruled out before initiating TARPEYO in patients who have spent time in the tropics or patients with unexplained diarrhea. Strongyloides Infestation Corticosteroids, including TARPEYO, should be discontinued in patients with known or suspected Strongyloides (threadworm) infestation. In such patients, corticosteroid-induced immunosuppression may lead to Strongyloides hyperinfection and dissemination with widespread larval migration, often accompanied by severe enterocolitis and potentially fatal gram-negative septicemia. Cerebral Malaria Avoid corticosteroids, including TARPEYO, in patients with cerebral malaria. Ocular Herpes Simplex Virus Infection Corticosteroids, including TARPEYO, may exacerbate ocular herpes simplex virus infections; therefore, avoid TARPEYO use in the presence of such infections. Kaposi's Sarcoma Kaposi's sarcoma has been reported to occur in patients receiving corticosteroid therapy, most often for chronic conditions. Discontinuation of corticosteroids may result in clinical improvement of Kaposi's sarcoma. Immunizations Corticosteroid therapy, including TARPEYO, may decrease the immune response to some vaccines. 5.3 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.

Side effects

The following clinically significant adverse reactions are described elsewhere in the labeling: Hypercorticism and adrenal axis suppression [see Warnings and Precautions ( 5.1 )] Risks of immunosuppression [see Warnings and Precautions ( 5.2 )] Other corticosteroid effects [see Warnings and Precautions ( 5.3 )] Most common adverse reactions ( ≥5%) are peripheral edema, hypertension, muscle spasms, acne, headache, upper respiratory tract infection, face edema, weight increased, dyspepsia, dermatitis, arthralgia, white blood cell count increased. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Calliditas Therapeutics at 1-844-IGA-0011 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials 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 safety of TARPEYO was evaluated in 389 patients in the randomized, double-blind, placebo-controlled study, NefIgArd (NCT: 03643965, Phase 3 clinical study in adults with primary IgAN). The data below reflect TARPEYO exposure in 195 patients with a median duration of 41 weeks, compared with comparable exposure to placebo in 194 patients. The most common adverse reactions, reported in greater than or equal to 5% of TARPEYO-treated patients and greater than or equal to 2% higher than placebo, in the 9-month treatment period are listed in Table 1 . Most adverse reactions that occurred at a greater incidence for TARPEYO compared to placebo were consistent with hypercortisolism and reversible, resolving within 3 months after discontinuation. Table 1: Reported adverse reactions occurring in greater than or equal to 5% of TARPEYO treated patients, and greater than or equal to 2% higher than Placebo Adverse Reaction TARPEYO 16 mg (N=195) Placebo (N=194) n (%) n (%) Peripheral edema 33 (17) 10 (5) Hypertension 23 (12) 6 (3) Muscle spasms 23 (12) 8 (4) Acne 22 (11) 2 (1) Headache 19 (10) 14 (7) Upper respiratory tract infection 16 (8) 12 (6) Face edema 15 (8) 1 (0.5) Weight increased 13 (7) 6 (3) Dyspepsia 13 (7) 4 (2) Dermatitis 12 (6) 2 (1) Arthralgia 12 (6) 4 (2) White blood cell count increased 11 (6) 1 (0.5)

Drug interactions

Potent CYP3A4 Inhibitors (e.g. ketoconazole, grapefruit juice): Can increase systemic budesonide concentrations: avoid concomitant use. ( 7.1 ) 7.1 Interaction with CYP3A4 Inhibitors Budesonide is a substrate for CYP3A4. Avoid use with potent CYP3A4 inhibitors; e.g. ketoconazole, itraconazole, ritonavir, indinavir, saquinavir, erythromycin, and cyclosporine [see Clinical Pharmacology ( 12.3 )] . Avoid ingestion of grapefruit juice with TARPEYO. Intake of grapefruit juice, which inhibits CYP3A4 activity, can increase the systemic exposure to budesonide [see Clinical Pharmacology ( 12.3 )] .

Use in specific populations

Lactation: Routine monitoring of linear growth in infants is recommended with chronic use of budesonide in the nursing mother. ( 8.2 ). 8.1 Pregnancy Risk Summary 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 IgA Nephropathy. Infants exposed to in utero corticosteroids, including budesonide, are at risk for hypoadrenalism (see Clinical Considerations ) . In animal reproduction studies with pregnant rats and rabbits, administration of subcutaneous budesonide during organogenesis at doses approximately 0.3 times or 0.03 times, respectively, the maximum recommended human dose (MRHD), resulted in increased fetal loss, decreased pup weights, and skeletal abnormalities. Maternal toxicity was observed in both rats and rabbits at these dose levels (see Data ) . The estimated background risk of major birth defects and miscarriage of the indicated population is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. 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/or Embryo/Fetal Risk IgA nephropathy in pregnancy is associated with adverse maternal outcomes, including increased rates of cesarean section, pregnancy-induced hypertension, pre-eclampsia and preterm delivery, and adverse fetal/neonatal outcomes, including stillbirth and low birth weight. Fetal/Neonatal Adverse Reactions Hypoadrenalism may occur in infants born to mothers receiving corticosteroids during pregnancy. Infants should be carefully observed for signs of hypoadrenalism, such as poor feeding, irritability, weakness, and vomiting, and managed accordingly [see Warnings and Precautions ( 5.1 )]. Data Animal Data Budesonide was teratogenic and embryo-lethal in rabbits and rats. In an embryo-fetal development study in pregnant rats dosed subcutaneously with budesonide during the period of organogenesis on gestation days 6 to 15 there were effects on fetal development and survival at subcutaneous doses up to approximately 500 mcg/kg in rats (approximately 0.3 times the maximum recommended human dose (MRHD) on a body surface area basis). In an embryo-fetal development study in pregnant rabbits dosed during the period of organogenesis on gestation days 6 to 18, there was an increase in maternal abortion, and effects on fetal development and reduction in litter weights at subcutaneous doses from approximately 25 mcg/kg (approximately 0.03 times the MRHD on a body surface area basis). Maternal toxicity, including reduction in body weight gain, was observed at subcutaneous doses of 5 mcg/kg in rabbits (approximately 0.006 times the maximum recommended human dose on a body surface area basis) and 500 mcg/kg in rats (approximately 0.3 times the maximum recommended human dose on a body surface area basis). In a peri- and post-natal development study, subcutaneous treatment of pregnant rats with budesonide during the period from Day 15 post coitum to Day 21 post partum, budesonide had no effects on delivery, but did have an effect on growth and development of offspring. In addition, offspring survival was reduced and surviving offspring had decreased mean body weights at birth and during lactation at exposures ≥ 0.012 times the MRHD (on a mg/m 2 basis at maternal subcutaneous doses of 20 mcg/kg/day and higher). These findings occurred in the presence of maternal toxicity. 8.2 Lactation Risk Summary Breastfeeding is not expected to result in significant exposure of the infant to TARPEYO. Lactation studies have not been conducted with oral budesonide, including TARPEYO, and no information is available on the effects of the drug on the breastfed infant or the effects of the drug on milk production. One published study reports that budesonide is present in human milk following maternal inhalation of budesonide (see Data ). Routine monitoring of linear growth in infants is recommended with chronic use of budesonide in the nursing mother. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for TARPEYO and any potential adverse effects on the breastfed infant from TARPEYO, or from the underlying maternal condition. Data One published study reports that budesonide is present in human milk following maternal inhalation of budesonide, which resulted in infant doses approximately 0.3% to 1% of the maternal weight-adjusted dosage and a milk to plasma ratio was approximately 0.5. Budesonide was not detected in plasma, and no adverse events were noted in the breastfed infants following maternal use of inhaled budesonide. Assuming a daily average milk intake of about 150 mL/kg/day and a milk to plasma ratio of 0.5, the estimated oral dose of budesonide for a 5 kg infant is expected to be less than 2 mcg/day for a maternal dose of 16 mg TARPEYO. Assuming 100% bio-availability in the infant this is about 0.1% of the maternal dose and about 3% of the highest inhaled dose used clinically for asthma in infants. 8.4 Pediatric Use The safety and efficacy of TARPEYO in pediatric patients have not been established. 8.5 Geriatric Use Clinical studies of TARPEYO did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Pregnancy

8.1 Pregnancy Risk Summary 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 IgA Nephropathy. Infants exposed to in utero corticosteroids, including budesonide, are at risk for hypoadrenalism (see Clinical Considerations ) . In animal reproduction studies with pregnant rats and rabbits, administration of subcutaneous budesonide during organogenesis at doses approximately 0.3 times or 0.03 times, respectively, the maximum recommended human dose (MRHD), resulted in increased fetal loss, decreased pup weights, and skeletal abnormalities. Maternal toxicity was observed in both rats and rabbits at these dose levels (see Data ) . The estimated background risk of major birth defects and miscarriage of the indicated population is unknown. All pregnancies have a background risk of birth defects, loss, or other adverse outcomes. 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/or Embryo/Fetal Risk IgA nephropathy in pregnancy is associated with adverse maternal outcomes, including increased rates of cesarean section, pregnancy-induced hypertension, pre-eclampsia and preterm delivery, and adverse fetal/neonatal outcomes, including stillbirth and low birth weight. Fetal/Neonatal Adverse Reactions Hypoadrenalism may occur in infants born to mothers receiving corticosteroids during pregnancy. Infants should be carefully observed for signs of hypoadrenalism, such as poor feeding, irritability, weakness, and vomiting, and managed accordingly [see Warnings and Precautions ( 5.1 )]. Data Animal Data Budesonide was teratogenic and embryo-lethal in rabbits and rats. In an embryo-fetal development study in pregnant rats dosed subcutaneously with budesonide during the period of organogenesis on gestation days 6 to 15 there were effects on fetal development and survival at subcutaneous doses up to approximately 500 mcg/kg in rats (approximately 0.3 times the maximum recommended human dose (MRHD) on a body surface area basis). In an embryo-fetal development study in pregnant rabbits dosed during the period of organogenesis on gestation days 6 to 18, there was an increase in maternal abortion, and effects on fetal development and reduction in litter weights at subcutaneous doses from approximately 25 mcg/kg (approximately 0.03 times the MRHD on a body surface area basis). Maternal toxicity, including reduction in body weight gain, was observed at subcutaneous doses of 5 mcg/kg in rabbits (approximately 0.006 times the maximum recommended human dose on a body surface area basis) and 500 mcg/kg in rats (approximately 0.3 times the maximum recommended human dose on a body surface area basis). In a peri- and post-natal development study, subcutaneous treatment of pregnant rats with budesonide during the period from Day 15 post coitum to Day 21 post partum, budesonide had no effects on delivery, but did have an effect on growth and development of offspring. In addition, offspring survival was reduced and surviving offspring had decreased mean body weights at birth and during lactation at exposures ≥ 0.012 times the MRHD (on a mg/m 2 basis at maternal subcutaneous doses of 20 mcg/kg/day and higher). These findings occurred in the presence of maternal toxicity.

Pediatric use

8.4 Pediatric Use The safety and efficacy of TARPEYO in pediatric patients have not been established.

Geriatric use

8.5 Geriatric Use Clinical studies of TARPEYO did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

Overdosage

Reports of acute toxicity and/or death following overdosage of corticoids are rare. In the event of acute overdosage, no specific antidote is available. Treatment consists of supportive and symptomatic therapy.

Description

(budesonide) delayed release capsules, for oral administration, contain budesonide, a synthetic corticosteroid, as the active ingredient. Budesonide is designated chemically as 16α, 17α-[(1RS)-Butylidenebis(oxy)]-11β, 21-dihydroxypregna-1,4-diene-3,20-dione. Budesonide is provided as a mixture of two epimers (22R and 22S). The empirical formula of budesonide is C 25 H 34 O 6 and its molecular weight is 430.5. Its structural formula is: Budesonide is a white to off-white, tasteless, odorless powder that is practically insoluble in water, sparingly soluble in alcohol, and freely soluble in chloroform. The beads in each capsule contain the following inactive ingredients: sugar spheres (sucrose and starch), hypromellose, polyethylene glycol, citric acid monohydrate, ethyl cellulose, medium chain triglycerides and oleic acid. The capsule shells contain hypromellose and titanium oxide (E171); and the printing ink on the capsules contain shellac, propylene glycol and black iron oxide (E172). The enteric coating on the capsules contain: methacrylic acid and methacrylate copolymer, talc and dibutyl sebacate. Structural Formula

Mechanism of action

12.1 Mechanism of Action Budesonide is a corticosteroid with potent glucocorticoid activity and weak mineralocorticoid activity that undergoes substantial first pass metabolism. Mucosal B-cells present in the ileum, including the Peyer's patches, express glucocorticoid receptors and are responsible for the production of galactose-deficient IgA1 antibodies (Gd-Ag1) causing IgA nephropathy. 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 TARPEYO's efficacy is mediated via local effects in the ileum vs systemic effects.

How supplied

(budesonide) delayed release capsules 4 mg, are white opaque- coated capsules marked with “CAL10 4 MG” in black ink on the body of the capsule. They are supplied as follows: NDC 81749-004-01: Bottles of 120 capsules. Child-resistant cap. Store at 20-25°C (68 - 77°F); excursions permitted to 15° to 30°C (59° to 86°F). [See USP Controlled Room Temperature]. Keep container tightly closed. Protect from moisture.

Patient information

Advise the patient to read the FDA-approved patient labeling ( Patient Information ). Advise patients that TARPEYO may cause hypercorticism and adrenal axis suppression and to follow a taper schedule, as instructed by their healthcare provider if discontinuing therapy [see Warnings and Precautions ( 5.1 )]. TARPEYO causes immunosuppression. Advise patients to avoid exposure to people with chicken pox or measles and, if exposed, to consult their healthcare provider immediately. There is an increased risk of developing a variety of infections, including worsening of existing tuberculosis, fungal, bacterial, viral or parasitic infections, or ocular herpes simplex, and to contact their healthcare provider if they develop any symptoms of infection [see Warnings and Precautions ( 5.3 )] . Provide advice regarding vaccination schedules for immunocompromised patients. Advise patients that TARPEYO delayed release capsules should be swallowed whole and not chewed, crushed or broken and to take TARPEYO in the morning, at least 1 hour before a meal [See Dosage and Administration ( 2 )]. Advise patients to avoid the consumption of grapefruit juice for the duration of their TARPEYO therapy [See Drug Interactions ( 7.1 )]. TARPEYO is a registered trademark of Calliditas Therapeutics AB, or its affiliates. © 2024 Calliditas Therapeutics AB (publ) Manufactured for and distributed by: Calliditas Therapeutics AB Stockholm, Sweden Patent: http://www.calliditas.com/patents

Label text from the FDA structured product label by Calliditas Therapeutics AB (revised Jan 21, 2026). Long sections are shortened; the complete label is on DailyMed.

Active ingredients

Budesonide in 1 product

Tarpeyo NDC products (1)

NDC	Strength & form	Labeler	Type
81749-004	Budesonide 4 mg/1 Capsule, Delayed Release	Calliditas Therapeutics AB	NDA

Frequently asked questions

What is Tarpeyo used for?

What are the side effects of Tarpeyo?

Who makes Tarpeyo?

Tarpeyo is listed by 1 labeler in the FDA NDC directory, including Calliditas Therapeutics AB.