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Evidence: MediumPeptideDiscontinuedCyclic polypeptideFDA-approved 1971 · discontinuedTuberculosis

Capreomycin

The injectable peptide that fell out of favour for drug-resistant tuberculosis

Capreomycin is a cyclic polypeptide antibiotic from Streptomyces bacteria, given by injection for multidrug-resistant tuberculosis. Approved in the US as Capastat in 1971 and now discontinued, it was a standard part of resistant-TB regimens until a large analysis linked it to worse outcomes.

Overview

What is it?

Capreomycin was for decades one of the injectable drugs used in combination regimens for multidrug-resistant tuberculosis (MDR-TB). It binds the bacterial ribosome and blocks protein synthesis. It had to be injected repeatedly for months, and like the aminoglycosides it is associated with kidney damage and hearing loss. It also disturbs blood salts: early reports described low potassium, magnesium and calcium in patients treated with it.

The evidence turned against it. A 2021 individual-patient meta-analysis of injectables in MDR-TB found capreomycin had been given to more patients than amikacin despite worse results: compared with capreomycin, amikacin was associated with 9 more cures and 5 fewer deaths per 100 patients treated, and streptomycin with 10 more cures and 10 fewer deaths.

In a 2017 UK cohort, hearing loss was about five times more likely with amikacin than with capreomycin alone, a reminder that both injectables carried real toxicity. In the US, Capastat is listed as discontinued. Researchers have explored inhaled capreomycin powders to reduce systemic toxicity, but none is approved.

Structured data

At a Glance

Every value in this table is printed from the Grey Peptides dataset, the same record the compound explorer and comparison tool read, so the three can never disagree.

ClassA cyclic polypeptide antibiotic produced by Streptomyces capreolus, given by injection for multidrug-resistant tuberculosis; approved in the US as Capastat in 1971, now discontinued, and no longer favoured after evidence linked it to worse outcomes.
US statusDiscontinued
Evidence levelMedium
Last reviewed2026-10-03
Evidence

Published Research

Studies of capreomycin, from their PubMed abstracts.

Human2021

Individual-patient meta-analysis of injectables

Across MDR-TB patients given injectables, capreomycin (2,401 patients) was used more than amikacin despite worse results: compared with capreomycin, amikacin was associated with 9 more cures and 5 fewer deaths per 100 patients, and streptomycin with 10 more cures and 10 fewer deaths.

PMID: 33124668
Human1970

Electrolyte disturbances

Tuberculosis patients treated with capreomycin developed gross electrolyte disturbances, including low potassium, magnesium and calcium and alkalosis, probably through secondary hyperaldosteronism; the authors advised withdrawing the drug if these developed.

PMID: 5489186
In Vitro2012

Pharmacokinetic model

An exploratory physiologically based pharmacokinetic model of capreomycin, a cyclic peptide antibiotic often grouped with the aminoglycosides, was built from targeted experimental data to predict its absorption, distribution and excretion.

PMID: 22143528
Human2017

Capreomycin vs amikacin side effects

In 100 UK patients, 55% had ototoxicity and 40% stopped the injectable for hearing loss; ototoxicity was about five times more likely in those started on amikacin than in those on capreomycin only.

PMID: 28696239
In Vitro2021

Inhaled capreomycin powder

A spray-dried inhaled powder of capreomycin was developed to target the lungs and reduce the systemic toxicity of repeated injections five times a week; it has not reached approval.

PMID: 34959328
In Vitro2005

Cross-resistance with other injectables

Analysis of resistant M. tuberculosis linked mutations in the 16S rRNA gene (rrs) and in tlyA to resistance to capreomycin, kanamycin, amikacin and viomycin, explaining variable cross-resistance among these injectables.

PMID: 16048924
Safety

Side Effects & Contraindications

Reported Side Effects

From the studies above.

● Hearing loss and kidney toxicity, as with other injectable anti-TB drugs
● Months of repeated injections

Contraindications & Cautions

No current US label: the product is discontinued and DailyMed has no manufacturer label (read October 3, 2026).

● Use only under specialist TB care where still available outside the US
Questions

Frequently Asked Questions

?Is capreomycin a peptide?

Yes. It is a cyclic polypeptide antibiotic produced by Streptomyces bacteria.

?Is capreomycin still used for tuberculosis?

It is discontinued in the US, and a 2021 individual-patient meta-analysis found capreomycin was associated with fewer cures and more deaths than amikacin or streptomycin.

?What are capreomycin's side effects?

Like other injectable TB drugs it can cause hearing loss and kidney damage; in a UK cohort, 40% of patients stopped their injectable because of hearing loss.

?How does tuberculosis become resistant to capreomycin?

Through mutations in the 16S ribosomal RNA gene or in tlyA, an enzyme that normally methylates the ribosome and makes the bacteria sensitive to capreomycin; some of these mutations also cause cross-resistance to amikacin and kanamycin.

Bibliography

References

  1. [fda] US FDA, Drugs@FDA (openFDA): CAPASTAT, NDA 050095 (June 2, 1971), marketing status discontinued; no manufacturer label on DailyMed. Read October 3, 2026.
  2. [pubmed] Arnold A, et al. "Adverse Effects and Choice between the Injectable Agents Amikacin and Capreomycin in Multidrug-Resistant Tuberculosis." Antimicrob Agents Chemother, 2017;61(9). PMID: 28696239.
  3. [pubmed] Shao Z, et al. "Spray-Dried Powder Formulation of Capreomycin Designed for Inhaled Tuberculosis Therapy." Pharmaceutics, 2021;13(12). PMID: 34959328.
  4. [pubmed] Maus CE, et al. "Molecular analysis of cross-resistance to capreomycin, kanamycin, amikacin, and viomycin in Mycobacterium tuberculosis." Antimicrob Agents Chemother, 2005;49(8):3192-7. PMID: 16048924.
  5. [clinical-trial] Cegielski JP, et al. "Aminoglycosides and Capreomycin in the Treatment of Multidrug-resistant Tuberculosis: Individual Patient Data Meta-analysis of 12 030 Patients From 25 Countries, 2009-2016." Clin Infect Dis, 2021;73(11):e3929-e3936. PMID: 33124668.
  6. [pubmed] Holmes AM, et al. "Capreomycin-induced serum electrolyte abnormalities." Thorax, 1970;25(5):608-11. PMID: 5489186.
  7. [pubmed] Reisfeld B, et al. "A physiologically based pharmacokinetic model for capreomycin." Antimicrob Agents Chemother, 2012;56(2):926-34. PMID: 22143528.

Sources & Citations

Studies were read from their PubMed records; regulatory sources are listed below, read October 3, 2026.

Medical Disclaimer: This content is for educational and informational purposes only. It is not medical advice, and nothing here is an instruction to obtain or use any compound. Consult a licensed healthcare provider before making health decisions.

Last reviewed: 2026-10-03