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Cabotegravir  Audio icon

Other Names: 744 LA, CAB, GSK-1265744, GSK1265744, GSK744, GSK744 LA, GSK744 LAP, S-265744, S/GSK1265744, cabotegravir LA, cabotegravir sodium
Drug Class: Integrase Inhibitors
Molecular Formula: C19 H17 F2 N3 O5
Registry Number: 1051375-10-0 (CAS)
Chemical Name: (3S,11aR)-N-((2,4-difluorophenyl)methyl)-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydrooxazolo(3,2-a)pyrido(1,2-d)pyrazine-8-carboxamide
Company: ViiV Healthcare
Phase of Development: Cabotegravir is in Phase IIb development for HIV treatment and Phase IIb/III development for HIV prevention.
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Chemical Image:
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cabotegravir
cabotegravir
Molecular Weight: 405.3553
(Compound details obtained from ChemIDplus Advanced,1 NIAID Therapeutics Database,2 and HIV i-BASE/Treatment Action Group 2016 Pipeline Report3)
Patent Version Content

Pharmacology


Mechanism of Action: HIV-1 integrase strand transfer inhibitor. Cabotegravir (CAB) prevents viral DNA integration into the host genome and is being developed for both HIV treatment and prevention.4,5

Half-life (T½): In a study of CAB (long-acting parenteral [LAP] nanosuspension administered via intramuscular [IM] or subcutaneous [SC] injection), the mean apparent terminal phase half-life ranged from 21 to 50 days. Following oral dosing, CAB half-life was 40 hours.6

Metabolism/Elimination: CAB is primarily metabolized via glucuronidation by UGT1A1 (main pathway) and UGT1A9 (minor pathway). CYP-mediated metabolism is expected to have a minimal role in CAB metabolism.7 Following a single oral radiolabeled dose of CAB 30 mg, 58.5% of the administered dose was recovered in feces and 26.8% was recovered in urine. CAB is eliminated in feces primarily as unchanged drug and in urine as a glucuronide metabolite (M1).8

Resistance: In vitro, CAB has exhibited activity against raltegravir-resistant isolates.9

Exposure of MT-2 cells infected with HIV-1 IIIB to increasing concentrations of CAB for up to 112 days did not produce highly resistant mutants. Among 25 site-directed molecular clones containing single INSTI-resistance substitutions, the majority remained fully susceptible to CAB. However, the Q148K and Q148R mutants resulted in a moderate loss of efficacy for CAB, with a 5.6-fold change (FC) with Q148K and a 5.1-FC with Q148R. Among 24 double or multiple integrase mutants, the following 6 had a FC >10 and were considered highly resistant to CAB: E138A/Q148R, E138K/Q148K, E138K/Q148R, G140C/Q148R, G140S/Q148R, and Q148R/N155H. CAB cross resistance to raltegravir and elvitegravir is limited. When tested against mutant viruses resistant to approved NRTIs, NNRTIs, and PIs, CAB demonstrated efficacy with a potency similar to that against wild-type virus.10,11

In vitro analysis was performed on the susceptibility of recombinant viruses with patient-derived integrase from various clades of HIV-1 to CAB. Fifty percent and 90% inhibitory concentrations (IC50 and IC90) of CAB against each virus was comparable to CAB’s activity against the wild-type control. No virus exhibited significant resistance to CAB. CAB demonstrated a modest reduction in activity against 2 common integrase-resistant viruses with the mutations G140S plus Q148H or E92Q plus N155H. These viruses, however, had significant resistance to raltegravir.12

In the Phase IIb LATTE study (NCT01641809), protocol-defined virologic failure (PDVF) was reported in 7 total participants (3 participants receiving oral CAB and 4 participants receiving efavirenz [EFV]) during the 24-week induction phase of the study. During the induction phase, no treatment-emergent resistance was detected. During the 72-week maintenance phase of the study, 5 total participants experienced PDVF: 2 in the CAB 10-mg group, 1 in the CAB 30-mg group, and 2 in the EFV group. Treatment-emergent resistance was detected in 3 participants, with 2 participants developing only NNRTI-resistance mutations and 1 participant (who had low CAB and rilpivirine [RPV] exposures) developing both an NNRTI (E138Q) and INSTI (Q148R) mutation.13,14

In the Phase IIb LATTE-2 study (NCT02120352), 3 participants (2 participants in the every-8-weeks dosing group and 1 participant in the oral dosing group) met PDVF criteria during the maintenance phase of the study. One of the participants experiencing PDVF in the every-8-weeks dosing group developed emergent RPV and CAB resistance. Genotypic testing found that the participant had NNRTI-resistance mutations (K103N, E138G, and K238T) and INSTI-resistance mutations (Q148R).15,16


Clinical Trials


Cabotegravir for HIV Treatment

Study Identifiers: LAI116482 (LATTE); NCT01641809
Sponsor: ViiV Healthcare
Phase: IIb
Study Purpose: The LATTE study is a dose-ranging efficacy study designed to select an oral dose of CAB and evaluate oral CAB plus RPV as a 2-drug ART regimen for suppressive maintenance therapy.
Study Population: Participants are HIV-infected, treatment–naive adults with HIV RNA ≥1,000 copies/mL at screening and CD4 counts ≥200 cells/mm3.
Dosing:
  • Induction phase: Participants will receive oral CAB 10, 30, or 60 mg once daily versus EFV 600 mg once daily, each given in combination with 2 background NRTIs. The induction phase will last through Week 24.
  • Maintenance phase: Those participants successfully completing the induction phase will continue their randomized dose of oral CAB, but will discontinue the background NRTIs and add RPV 25 mg. The comparator arm will continue with EFV 600 mg plus the background NRTIs. The maintenance phase will last through Week 96.
  • Open-Label phase: Participants receiving oral CAB + RPV in the maintenance phase will be allowed to continue treatment on the same regimen beyond Week 96.13,14,17,18

Selected Study Results:

Study Identifiers: LATTE-2; NCT02120352
Sponsor: ViiV Healthcare
Phase: IIb
Study Purpose: LATTE-2 is an open-label safety and efficacy study to (1) evaluate the antiviral activity, tolerability, and safety of 2 intramuscular (IM) dosing regimens of the long-acting injectables CAB LA plus RPV LA relative to oral CAB plus abacavir/lamivudine (ABC/3TC) as maintenance therapy, and (2) select an IM regimen of CAB LA plus RPV LA for progression into Phase III trials.
Study Population: Participants are HIV-infected, treatment-naive adults with HIV RNA ≥1,000 copies/mL at screening and CD4 counts ≥200 cells/mm3.
Dosing:
  • Induction phase: Participants will receive a once-daily regimen of oral CAB 30 mg + ABC/3TC 600/300 mg for 20 weeks. In the last 4 weeks of the induction phase, participants will also receive oral RPV 25 mg once daily. (Participants with HIV-1 RNA <50 copies/mL will continue on to the maintenance phase of the study.)
  • Maintenance phase: Following induction, qualifying participants will be randomized to 1 of the 3 treatment arms below for maintenance therapy. All doses of CAB LA and RPV LA will be given IM.
    • Q4W dosing group: Participants will receive a loading dose of CAB LA 800 mg + RPV LA 600 mg on Day 1. Starting at Week 4, participants will receive a regimen of CAB LA 400 mg + RPV LA 600 mg, administered every 4 weeks until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if continuing to extension phase).
    • Q8W dosing group: A loading dose of CAB LA 800 mg + RPV LA 900 mg will be given on Day 1. A second loading dose of CAB LA 600 mg will be given at Week 4. Starting at Week 8, participants will receive a regimen of CAB LA 600 mg + RPV LA 900 mg, administered every 8 weeks until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if continuing to extension phase).
    • Oral dosing group: Participants will receive oral CAB 30 mg + ABC/3TC administered daily until Week 32 (primary endpoint). Treatment will continue until Week 96 (or longer if electing to receive IM treatment during the extension phase).
  • Extension phase: For long-term collection of efficacy and safety data.
There will also be a long-term follow-up period for participants who withdraw from the study and have received at least 1 dose of CAB LA and/or RPV LA.15,16,19-22
Selected Study Results:

Cabotegravir for HIV Prevention

Study Identifiers: ECLAIR; NCT02076178
Sponsor: ViiV Healthcare
Phase: IIa
Study Purpose: The ECLAIR study evaluated the safety, tolerability, and acceptability of CAB LA for pre-exposure prophylaxis (PrEP).
Study Population: Participants were HIV-uninfected, adult males who were at low risk of acquiring HIV.
Dosing:
  • Oral Phase: Participants initially received oral CAB 30 mg or placebo once daily for 4 weeks.
  • Injection Phase: Following a 1-week washout period, participants then received CAB LA 800 mg or placebo, administered by IM injection once every 12 weeks for 3 cycles.
Follow-up continued for 40 weeks after the Week 41 primary endpoint.23-27
Selected Study Results:
Another Phase IIa study (HPTN 077; NCT02178800) is evaluating the safety, tolerability, and pharmacokinetics of CAB LA in HIV-uninfected women and men.28 In addition, the Phase IIb/III HPTN 083 study (NCT02720094) is evaluating the safety and effectiveness of CAB LA compared to oral tenofovir DF/emtricitabine for PrEP in HIV-uninfected men and transgender women, both of whom have sex with men and are at high risk of acquiring HIV infection.29


Adverse Events


LATTE Study (NCT01641809)
In the Week 96 analysis of the LATTE study involving 243 treatment-naive participants (n = 181 CAB; n = 62 EFV), drug-related adverse events (AEs) ≥Grade 2 occurred in 14% of participants in the oral CAB arm and in 19% of participants in the EFV arm, overall. Drug-related AEs ≥Grade 2 occurring during the 72-week maintenance phase were reported in 4% of oral CAB participants and 4% of EFV participants. Headache was more common with oral CAB treatment than with EFV treatment.

Serious adverse events (SAEs) occurred in 10% of participants receiving oral CAB and 6% of participants receiving EFV, with none of the SAEs in the oral CAB groups deemed drug-related and one of the SAEs in the EFV group considered drug-related. Three percent of oral CAB participants versus 15% of EFV participants withdrew from the study because of an AE (with most withdrawals occurring prior to the maintenance phase).

Grade 3-4 laboratory abnormalities occurred in 26% of participants assigned to oral CAB versus 37% of participants assigned to EFV, most commonly due to elevated CPK. Elevations in ALT (any grade) occurred in 20% of oral CAB participants and 21% of EFV participants.13,14,30

LATTE-2 Study (NCT02120352)
In the LATTE-2 study involving 309 participants, 286 participants were randomized to maintenance therapy (n = 115 IM CAB every 8 weeks; n = 115 IM CAB every 4 weeks; n = 56 oral CAB). Week 48 results found that overall, among participants receiving IM treatment (CAB LA or RPV LA), the most common injection site reactions (ISRs) were pain (67%), nodules (7%), and swelling (6%). The majority of ISRs were mild (82%) or moderate (17%) in severity and most resolved within 7 days. Two participants (in the every-8-weeks dosing group) withdrew from the study because of an ISR.

During the maintenance phase, drug-related AEs (excluding ISRs) occurring in ≥3% of participants in any of the treatment groups (IM groups or oral CAB group) included pyrexia, fatigue, influenza-like illness, headache, and rash. Drug-related Grade 3 or 4 AEs (excluding ISRs) occurred in 2 participants in the every-8-weeks group (influenza-like illness, chills, and pain), 4 participants in the every-4-weeks group (influenza-like illness, rash, depression, and psychosis), and 0 participants in the oral CAB group.

Seven percent of participants in the IM dosing groups and 5% of participants in the oral dosing group experienced an SAE during the maintenance phase, but none were drug-related. Nine participants in the IM dosing groups and 1 participant in the oral CAB group withdrew from the study during the maintenance phase because of an AE. Treatment-emergent lab abnormailites ≥Grade 3 during the maintenance period occurred in 18% of participants in the IM dosing groups and in 16% of participants in the oral dosing group. 

A Week 32 analysis of satisfaction, tolerability, and acceptability of CAB LA plus RPV LA found that the majority of participants receiving CAB LA reported overall satisfaction with their treatment and were willing to continue with LA treatment beyond Week 32. On items related to convenience, flexibility, and lifestyle, participants were more satisfied with CAB LA than with oral CAB.15,16,22

ECLAIR Study (NCT02076178)
In the 41-week ECLAIR study involving a total of 126 treated participants (n = 105 CAB; n = 21 placebo), 18 participants withdrew from CAB during the study: 5 during oral therapy, 6 after oral therapy but prior to injections, and 7 during the injection period. During the injection phase, 4 out of 94 participants receiving CAB LA withdrew from the study because of injection intolerability. During the oral phase, 7 participants withdrew because of CAB-related AEs, which included 3 events of neutropenia, 3 events of increased blood CPK, and 1 event of fatigue. One participant receiving CAB LA experienced an SAE (appendicitis).

Overall, Grade 2 to 4 AEs occurred in 62% of placebo participants and 80% of CAB participants. During the injection phase, Grade 2 to 4 AEs (occurring in >5% of participants in the CAB LA arm) were reported in 80% of participants receiving CAB LA versus 48% of participants receiving placebo. The most common Grade 2 to 4 AE in the CAB LA group was injection site pain, followed by pyrexia, injection site pruritus, and injection site swelling. An analysis of ISRs occurring during the injection phase of the study found that 57% of participants in the placebo group experienced ISRs, whereas 93% of participants in the CAB LA group experienced ISRs. The majority of ISRs were Grade 1 or 2 in severity.

Grade 2 to 4 drug-related lab abnormalities occurred in 13% of CAB participants versus 5% of placebo participants. A majority of CAB LA participants reported satisfaction with side effects related to study medication. On items related to convenience, flexibility, and lifestyle, participants were more satisfied with CAB LA than with oral CAB.23-27


Drug Interactions


Oral CAB does not affect the pharmacokinetics of midazolam in human study participants, indicating that CAB is neither a CYP inhibitor nor inducer. In vitro, CAB does not inhibit UGT enzymes, except UGT1A3. (CAB, however, is predicted to have no clinically significant effect on UGT1A3 substrates.) CAB does not inhibit hepatic, intestinal, or renal drug transporters, except for OAT1 and OAT3 (OAT1/3). Drug-drug interactions are possible between CAB and sensitive OAT1/3 substrates having a narrow therapeutic index (such as methotrexate).7,31

Coadministration of oral CAB with an oral contraceptive containing levonorgestrel (LNG) and ethinyl estradiol (EE) did not affect the pharmacokinetics of LNG or EE, suggesting oral CAB can be administered in combination with LNG- and EE-containing oral contraceptives without clinically significant interactions.32

There are no apparent pharmacokinetic interactions between oral CAB and etravirine or between oral CAB and RPV.33,34

Coadministration of steady-state rifampin (RIF) 600 mg with a single-dose of oral CAB 30 mg increased CAB oral clearance by 2.4-fold and decreased CAB AUC(0-∞) by 59% compared to CAB administered alone. The coadministration of RIF with oral CAB 30 mg once daily is not recommended. Coadministration of RIF with CAB LA is also not recommended until further study is completed.35


References


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Last Reviewed: November 1, 2016

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