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Rukobia

Last reviewed on RxList: 7/13/2020
Rukobia Side Effects Center

Medical Editor: John P. Cunha, DO, FACOEP

What Is Rukobia?

Rukobia (fostemsavir), is a human immunodeficiency virus type 1 (HIV-1) gp120-directed attachment inhibitor, used in combination with other antiretroviral(s), to treat HIV-1 infection in heavily treatment-experienced adults with multidrug-resistant HIV-1 infection failing their current antiretroviral regimen due to resistance, intolerance, or safety considerations.

What Are Side Effects of Rukobia?

Side effects of Rukobia include:

  • nausea,
  • diarrhea,
  • headache,
  • abdominal pain,
  • indigestion/heartburn,
  • fatigue,
  • rash,
  • sleep disturbance,
  • immune reconstitution inflammatory syndrome,
  • drowsiness, and
  • vomiting

Dosage for Rukobia

The dose of Rukobia is one tablet taken twice daily with or without food.

Rukobia In Children

The safety and effectiveness of Rukobia have not been established in pediatric patients.

What Drugs, Substances, or Supplements Interact with Rukobia?

Rukobia may interact with other medicines such as:

Tell your doctor all medications and supplements you use.

Rukobia During Pregnancy and Breastfeeding

Tell your doctor if you are pregnant or plan to become pregnant before using Rukobia; it is unknown how it would affect a fetus. There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to Rukobia during pregnancy. It is unknown if Rukobia passes into breast milk. Breastfeeding is not recommended due to the potential for HIV-1 transmission.

Additional Information

Our Rukobia (fostemsavir) Extended-Release Tablets, for Oral Use Side Effects Drug Center provides a comprehensive view of available drug information on the potential side effects when taking this medication.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

QUESTION

What is HIV? See Answer
Rukobia Professional Information

SIDE EFFECTS

The following adverse reactions are discussed in greater detail in other sections of the labeling:

  • Immune reconstitution syndrome [see WARNINGS AND PRECAUTIONS].
  • QTc prolongation [see WARNINGS AND PRECAUTIONS].
  • Elevations in hepatic transaminases in patients with hepatitis B or C virus co-infection [see WARNINGS AND PRECAUTIONS].

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 with rates in the clinical trials of another drug and may not reflect the rates observed in practice.

A total of 620 subjects with HIV-1 infection received at least one dose of RUKOBIA as part of a controlled clinical trial.

The primary safety assessment of RUKOBIA is based on 96 weeks of data from a Phase 3 partially randomized, international, multicenter, double-blind, placebo-controlled trial (BRIGHTE) conducted in 371 heavily treatment-experienced adult subjects [see Clinical Studies]. In the randomized cohort, 203 subjects received at least one dose of blinded RUKOBIA 600 mg twice daily and 69 subjects received placebo in addition to their current failing regimen for 8 days of functional monotherapy. Beyond Day 8, all randomized subjects except one received open-label RUKOBIA 600 mg twice daily plus an optimized background therapy (OBT). In the nonrandomized cohort, 99 subjects received open-label RUKOBIA 600 mg twice daily plus OBT from Day 1 onward.

A total of 370 subjects (271 randomized and 99 nonrandomized) received at least 1 dose of RUKOBIA 600 mg twice daily in the BRIGHTE trial. Overall, most (81%) of the adverse reactions reported with RUKOBIA were mild or moderate in severity. The proportion of subjects who discontinued treatment with RUKOBIA due to an adverse event was 7% at Week 96 (randomized: 5% and nonrandomized: 12%). The most common adverse events leading to discontinuation were related to infections (3% of subjects receiving RUKOBIA). Serious drug reactions occurred in 3% of subjects and included 3 cases of severe immune reconstitution inflammatory syndrome.

Data from the randomized cohort form the basis of the safety assessment of RUKOBIA because the presence of significant comorbid illness in the nonrandomized cohort (associated with advanced HIV infection) may confound the assessment of causality. Adverse reactions (all grades) reported in ≥2% of subjects in the randomized cohort in the Week 96 analysis are listed in Table 1.

Table 1. Adverse Reactionsa (Grades 1 to 4) Reported in ≥2% of Subjects Receiving RUKOBIA plus OBT in the BRIGHTE Trial, Randomized Cohort (Week 96 Analysis)

Adverse ReactionRUKOBIA plus OBT
(n = 271)b
Nausea10%
Diarrhea4%
Headache4%
Abdominal painc3%
Dyspepsia3%
Fatigued3%
Rashe3%
Sleep disturbancef3%
Immune Reconstitution Inflammatory Syndrome2%
Somnolence2%
Vomiting2%
a Frequencies of adverse reactions are based on all treatment-emergent adverse events attributed to study drug by the investigator.
b Of the 272 subjects enrolled in the randomized cohort, 1 subject who received placebo withdrew from the trial prior to receiving RUKOBIA in the open-label phase of the trial.
c Includes pooled terms: abdominal discomfort, abdominal pain, and abdominal pain upper.
d Includes pooled terms: fatigue and asthenia.
e Includes pooled terms: rash, rash generalized, rash maculo-papular, rash pruritic, and dermatitis allergic.
f Includes pooled terms: insomnia, sleep deficit, sleep disorder, abnormal dreams.

Adverse reactions in the nonrandomized cohort were similar to those observed in the randomized cohort. The most common adverse reactions reported in nonrandomized subjects were fatigue (7%), nausea (6%), and diarrhea (6%).

Less Common Adverse Reactions

The following adverse reactions occurred in <2% of subjects receiving RUKOBIA in the randomized cohort of the BRIGHTE trial. These events have been included based on the assessment of potential causal relationship and were also reported in the nonrandomized cohort.

Cardiac Disorders: Electrocardiogram QT prolonged. All reports were asymptomatic.

Musculoskeletal Disorders: Myalgia.

Nervous System Disorders: Dizziness, dysgeusia, neuropathy peripheral (includes pooled terms:neuropathy peripheral and peripheral sensory neuropathy).

Skin and Subcutaneous Tissue Disorders: Pruritus.

Laboratory Abnormalities

Selected laboratory abnormalities (Grades 3 to 4) with a worsening grade from baseline and representing the worst-grade toxicity in ≥2% of subjects in the randomized cohort of the BRIGHTE trial are presented in Table 2.

Table 2. Selected Laboratory Abnormalities (Grades 3 to 4) Reported in ≥ 2% of Subjects in the Randomized Cohort Receiving RUKOBIA plus OBT in the BRIGHTE Trial (Week 96 Analysis)

Laboratory Parameter Preferred TermRUKOBIA plus OBT
(n = 271a)
ALT (>5.0 x ULN)5%
AST (>5.0 x ULN)4%
Direct bilirubin (>ULN)b7%
Bilirubin ( ≥2.6 x ULN)3%
Cholesterol (≥300 mg/dL)b5%
Creatinine (>1.8 x ULN or 1.5 x baseline)19%
Creatine kinase (≥10 x ULN)2%
Hemoglobin (<9.0 g/dL)6%
Hyperglycemia (>250 mg/dL)4%
Lipase (>3.0 x ULN)5%
LDL cholesterol (≥190 mg/dL)4%
Neutrophils (≤599 cells/mm3 )4%
Triglycerides (>500 mg/dL)5%
Urate (>12 mg/dL)3%
ULN = Upper limit of normal.
a Percentages were calculated based on the number of subjects with post-baseline toxicity grades for each laboratory parameter (n = 221 for cholesterol and triglycerides, n = 216 for LDL cholesterol, and n = 268 for all other parameters).
b Grade 3 only (no Grade 4 values reported).

The incidence of selected laboratory abnormalities (Grades 3 to 4) in the nonrandomized cohort were overall consistent with those of the randomized cohort, with the exception of direct bilirubin (14% versus 7%), bilirubin (6% versus 3%), lipase (10% versus 5%), triglycerides (10% versus 5%), neutrophils (7% versus 4%), and leukocytes (6% versus 1%), respectively.

Changes in Serum Creatinine

Clinically relevant increases in serum creatinine have primarily occurred in patients with identifiable risk factors for reduced renal function, including preexisting medical history of renal disease and/or concomitant medications known to cause increases in creatinine. A causal association between RUKOBIA and elevation in serum creatinine has not been established.

Changes in Direct Bilirubin

Increases in direct (conjugated) bilirubin have been observed following treatment with RUKOBIA (Table 2). Cases of clinical significance were uncommon and were confounded by the presence of intercurrent serious comorbid events (e.g., sepsis, cholangiocarcinoma, or other complications of viral hepatitis co-infection). In the remaining cases, elevations in direct bilirubin (without clinical jaundice) were typically transient, occurred without increases in liver transaminases, and resolved on continued RUKOBIA.

Changes in ALT and AST in Subjects with Hepatitis B and/or Hepatitis C Virus Co-infection

A total of 29 subjects with Hepatitis B and/or Hepatitis C co-infection were enrolled in the BRIGHTE trial (randomized and nonrandomized cohorts combined). Grade 3 and 4 elevations in ALT and AST occurred in 14% of these subjects compared with 3% (ALT) and 2% (AST) of subjects without viral hepatitis co-infection. Some of these elevations in transaminases were consistent with hepatitis B reactivation particularly in the setting where anti-hepatitis therapy was withdrawn [see WARNINGS AND PRECAUTIONS].

Read the entire FDA prescribing information for Rukobia (Fostemsavir Extended-release Tablets)

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© Rukobia Patient Information is supplied by Cerner Multum, Inc. and Rukobia Consumer information is supplied by First Databank, Inc., used under license and subject to their respective copyrights.

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